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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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28-03-2013 дата публикации

Complexes of Ruthenium, Method of Production Thereof And Use Thereof As (Pre)Catalysts of the Metathesis Reaction

Номер: US20130079515A1
Автор: BARBASIEWICZ Michal, GRELA Karol, SZADKOWSKA Anna
Принадлежит: UMICORE AG & CO. KG

The present invention provides ruthenium complexes of the formula 111-. (canceled)13. The complex of claim 12 , wherein X and X′ are chlorine.14. The complex of claim 12 , wherein Ris hydrogen.15. The complex of claim 12 , wherein A is nitrogen.16. The complex of claim 12 , wherein A is carbon with an Rgroup.17. The method for preparing the ruthenium complex of which comprises reacting 8-ethenylquinoline with a Ru carbene catalyst.19. The method of claim 17 , wherein the Ru carbene catalyst comprises an indenylidene residue claim 17 ,20. The method according to claim 17 , wherein the reaction is conducted in the presence of a copper(I) salt.21. The method according to claim 20 , wherein the copper(I) salt is copper(I) chloride.22. The method according to claim 17 , wherein the reaction is performed in a chlorinated solvent claim 17 , an aliphatic solvent claim 17 , a cycloaliphatic solvent or an aromatic hydrocarbon solvent claim 17 , or mixtures thereof.24. An improved process for ring closing metathesis (RCM) claim 12 , wherein the improvement comprise the use of the ruthenium complex of as an initiator or (pre)catalyst.25. An improved process for ring-opening metathesis polymerization (ROMP) claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst.26. An improved process for metathesis of “alkene-alkyne” (ene-yne) type claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst. This application is a continuation application of U.S. patent application Ser. No. 12/303,615, filed Apr. 3, 2009, which in turn is a national stage application of PCT Application No. EP2007/004901, filed Jun. 1, 2007. The disclosures of the above-referenced applications are hereby incorporated by reference into the present disclosure.The invention relates to novel metal complexes with formula 1, whereCompounds of formula 1 occur as two isomers: with formula 1a, in which atoms X ...

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Номер записи: 1
25-04-2013 дата публикации

SUBSTITUTED BIARYL ALKYL AMIDES

Номер: US20130102649A1
Автор: Chan Kyle W.H., Mercurio Frank, Stirling David I.
Принадлежит: BioTheryX, Inc.

Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds. 2. The compound of claim 1 , wherein n is selected from the group consisting of 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , and 5.3. The compound of claim 2 , wherein n is 2.4. The compound of claim 1 , wherein each Ris halo.5. The compound of claim 4 , wherein each Ris chloro.6. The compound of claim 1 , wherein Z claim 1 , Z claim 1 , Zand Zare each —CH—.7. The compound of claim 1 , wherein Ris (Calkoxy)Calkyl.8. The compound of claim 7 , wherein Ris methoxymethyl or ethoxymethyl.9. The compound of claim 1 , wherein Ris (aryloxy)Calkyl.10. The compound of claim 9 , wherein Ris phenoxymethyl.11. The compound of claim 1 , wherein Ris Cheterocyclyl.12. The compound of claim 11 , wherein Ris selected from optionally substituted tetrahydrofuranyl or optionally substituted pyrrolidinyl.13. The compound of claim 12 , wherein the nitrogen atom in pyrrolidinyl is protected with a t-butyloxycarbonyl (Boc) protecting group.14. The compound of claim 1 , wherein Ris Ccycloalkyl.15. The compound of claim 14 , wherein Ris cyclopentyl.16. The compound of claim 1 , wherein Ris haloalkyl.17. The compound of claim 16 , wherein Ris selected from the group consisting of —CHCl claim 16 , —CHBr claim 16 , —CHCHCl claim 16 , —CHCHBr claim 16 , —CH(Cl)CHand —CH(Br)CH.18. The compound of claim 1 , wherein Ris optionally substituted aminoalkyl.19. The compound of claim 18 , wherein Ris selected from the group consisting of —CHNH claim 18 , —CHNH(Boc) claim 18 , —CH(NH)CH claim 18 , and —CH(Boc-NH)CH.20. The compound of claim 1 , wherein Ris —OH.22. The compound of claim 21 , wherein Ris —OH.23. The compound of claim 1 , wherein Ris selected from the group consisting of —OH claim 1 , —NHR claim 1 , an optionally substituted Calkoxy claim 1 , and an optionally ...

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Номер записи: 2
27-06-2013 дата публикации

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Номер: US20130165649A1
Автор: Cazin Catherine
Принадлежит:

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

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Номер записи: 3
11-07-2013 дата публикации

Process for preparation of substantially pure fosamprenavir calcium and its intermediates

Номер: US20130174651A1
Автор: Gaurav Kumar, Girij Pal Singh, Purna Chandra Ray, Samir Shanteshwar Shabade, Surinder Kumar Arora
Принадлежит: Lupin Ltd

The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R) tetrahydro -3 -furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.

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Номер записи: 4
01-08-2013 дата публикации

METHODS AND COMPOUNDS USEFUL IN THE SYNTHESIS OF FUSED AMINODIHYDROTHIAZINE DERIVATIVES

Номер: US20130197244A1
Автор: Farthing Christopher N., Kim Dae-Shik, Mitasev Branko, Schnaderbeck Matthew J., Zhang Huiming
Принадлежит: Eisai R&D Management Co., Ltd.

Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme. 111.-. (canceled)13. The compound of claim 12 , wherein the oxygen protecting group is selected from the group consisting of: Trt (triphenylmethyl) claim 12 , MPM (p-methoxybenzyloxymethyl) claim 12 , TBDMS (t-butyldimethylsilyl) claim 12 , and TBDPS (t-butyldiphenyl silyl) claim 12 ,or a salt thereof.14. The compound of claim 12 , wherein:{'sub': '1', 'Ris trifluoromethyl, hydroxymethyl, monofluoromethyl, or triphenylmethoxymethyl,'}or a salt thereof.15. The compound of claim 12 , wherein:{'sub': '1', 'Ris trifluoromethyl, hydroxymethyl, monofluoromethyl, or triphenylmethoxymethyl;'}{'sub': '2', 'Ris fluoro; and'}{'sub': '3', 'Ris hydrogen or fluoro,'}or a salt thereof.18. The method of claim 17 , wherein said stereochemically pure compound has greater than about 90% by weight of one stereoisomer of the compound and less than about 10% by weight of the other stereoisomers of the compound.19. The method of claim 17 , wherein said stereochemically pure compound has greater than about 97% by weight of one stereoisomer of the compound and less than about 3% by weight of the other stereoisomers of the compound.20. The method of claim 17 , wherein said crystallizing step is performed by cooling the mixture of diastereomeric salts of the compound of Formula II.21. The method of claim 20 , wherein said cooling is from a temperature of from 40° C. to 80° C. claim 20 , to a temperature of from −10° C. to 29° C.22. The method of claim 17 , wherein the solvent is an alcohol.23. The method of claim 17 , wherein the solvent is ethanol.24. The method of claim 17 , wherein the solvent is a mixture of two or more solvents.25. The method of claim 24 , wherein the mixture is a toluene-acetonitrile mixture claim 24 , a toluene-acetone mixture claim 24 , a toluene-tetrahydrofuran mixture claim 24 , or an alcohol-water mixture.26. ...

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Номер записи: 5
22-08-2013 дата публикации

Selective Androgen Receptor Modulators

Номер: US20130217762A1
Автор: GREEN Jonathan Edward, JADHAV Prabhakar Kondaji, Krishnan Venkatesh, MATTHEWS Donald Paul, SAEED Ashraf, STEPHENSON Gregory Alan
Принадлежит: ELI LILLY AND COMPANY

The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof. 6. A compound of that is 2-chloro-4-[[(1R claim 5 ,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile.8. A compound of that is 2-Chloro-4-[[(1S claim 7 ,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile.9. A pharmaceutical composition comprising a compound of any of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients.10. A pharmaceutical composition comprising a compound of any of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , and one or more pharmaceutically acceptable carriers claim 5 , diluents claim 5 , or excipients.11. A pharmaceutical composition comprising a compound of any of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , and one or more pharmaceutically acceptable carriers claim 7 , diluents claim 7 , or excipients.12. A pharmaceutical composition according to which is formulated as a patch.13. A pharmaceutical composition according to which is formulated as a topical gel.14. A pharmaceutical composition according to which is formulated as a topical cream.15. A pharmaceutical composition according to which is formulated as a topical spray.16. A pharmaceutical composition according to comprising a solvate.17. A pharmaceutical composition according to which is 2-chloro-4-[[(1R claim 16 ,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile•ethanol solvate in crystalline form characterized by an X-ray powder diffraction pattern obtained from a CuKα source (λ=X Å) which comprises peaks at:a) 7.00, 17.26, 12.30, and 23.34+/−−0.2 in 2θ; orb) 7.00, 8.59, 12.30, 16.76, 17.26, and 23.34+/−−0.2 in 2θ; orc) 7.00, 8.59, 10.13, 11.89, 12.30, 12.91, 13.95, 16.76, 17.26, 23.34+/−−0.2 in 2θ.18. A method for the treatment of muscle atrophy in a patient ...

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Номер записи: 6
29-08-2013 дата публикации

Metathesis Catalysts Containing Onium Groups

Номер: US20130225807A1
Автор: Krzysztof Skowerski, Lukasz Gulajski, Michal Bieniek
Принадлежит: Apeiron Synthesis Sp zoo

Disclosed herein is a general method for the preparation of complexes containing a quaternary onium group in an inert ligand. Some of these complexes may be represented by formula 1: Methods for the preparation of complexes of formula 1, the preparation of intermediates and the use of complexes of formula 1 in metathesis reactions and a method for conducting an olefin metathesis reaction are also described.

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Номер записи: 7
29-08-2013 дата публикации

METHOD FOR PREPARING ALISKIREN AND ITS INTERMEDIATES THEREOF

Номер: US20130225841A1
Автор: Cheng Rongde, Peng Lingchao, Tu Yongjun, Zhang Yi
Принадлежит: Zhejiang Tianyu Pharmaceutical Co., Ltd.

A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing Rfrom the amino group and obtaining Aliskiren shown as formula I. 2. The method according to wherein the ether class solvent in step (1) is one selected from diethyl ether claim 1 , tetrahydrofuran or 1 claim 1 ,2-dimethoxyethane.3. The method according to wherein the inert solvent in step (2) is methylene chloride or tetrahydrofuran.4. The method according to wherein the ketone class solvent in step (3) is acetone or 2-butanone; and the molar ratio between lithium bromide and the compound of formula XX is 1.1 to 5.5. The method according to wherein the said ether class solvent in step (4) is either one or mixture of any two selected from diethyl ether claim 1 , tetrahydrofuran or 1 claim 1 ,2-dimethoxyethane; the said iron-contained catalyst is selected from iron(III) acetylacetonate or Iron(III) chloride; and the reaction temperature is −15° C.˜20° C.7. The method according to for preparing the Aliskiren compound of formula I claim 6 , wherein the reaction in step (a) between the compound of formula XV and the compound of formula VII to obtain the compound of formula XXIII is implemented in an inert solvent.8. The method according to for preparing the Aliskiren compound of formula I claim 7 , wherein the inert solvent is one selected from dioxane or toluene.9. ...

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Номер записи: 8
12-09-2013 дата публикации

Intermediates useful for the synthesis of fexofenadine, processes for their preparation and for the preparation of fexofenadine

Номер: US20130237709A1
Автор: Graziano Castaldi, Marco Baratella, Mauro Gaboardi
Принадлежит: CHEMELECTIVA Srl

Intermediates useful for the synthesis of fexofenadine, processes for their preparation and processes for the synthesis of fexofenadine are described.

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Номер записи: 9
12-09-2013 дата публикации

INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B

Номер: US20130237711A1
Автор: Benayoud Farid, Calkins Trevor Lee, Chase Charles E., Christ William, Fang Francis G.
Принадлежит: Eisai R&D Management Co., Ltd.

Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided. 8. The compound of claim 1 , wherein the compound is of formula C claim 1 , and Ris methyl.10. The compound of claim 9 , wherein said suitable hydroxyl protecting group claim 9 , taken with the oxygen atom to which it is bound claim 9 , is selected from an ester claim 9 , a silyl ether claim 9 , an alkyl ether claim 9 , an arylalkyl ether claim 9 , and an alkoxyalkyl ether.11. The compound of claim 9 , wherein said suitable leaving group is selected from the group consisting of sulphonyloxy claim 9 , optionally substituted alkylsulphonyloxy claim 9 , optionally substituted alkenylsulfonyloxy claim 9 , optionally substituted arylsulfonyloxy claim 9 , and halogen. This application is a continuation of U.S. application Ser. No. 13/476,276, filed May 21, 2012, which is a continuation of U.S. application Ser. No. 13/171,971, filed Jun. 29, 2011, which is a continuation of U.S. application Ser. No. 11/628,396, filed Mar. 28, 2007 (U.S. Pat. No. 7,982,060), which claims priority under 35 U.S.C. §371 from International Application No. PCT/US05/019669, filed Jun. 3, 2005, which claims benefit of U.S. Provisional Patent Application Nos. 60/576,642, filed Jun. 3, 2004, 60/626,769, filed Nov. 10, 2004, and 60/663,300 filed Mar. 18, 2005, the entire contents of each of which are incorporated herein by reference.The present invention relates to compounds useful as intermediates in the synthesis of pharmaceutically active macrolide compounds.The invention relates to pharmaceutically active macrolides, synthesis thereof and intermediates thereto. Halichondrin B is a potent anticancer agent originally isolated from the marine sponge , and subsequently found in sp., , and sp. A total synthesis of Halichondrin B was published in 1992 (Aicher, T. D. et al., 114:3162-3164). Halichondrin B has demonstrated in vitro inhibition of tubulin polymerization, microtubule assembly, beta-tubulin ...

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Номер записи: 10
19-09-2013 дата публикации

PROCESS FOR THE PREPARATION OF (3R, 3AS, 6AR)-HEXAHYDROFURO [2, 3- B] FURAN-3-OL

Номер: US20130244297A1
Автор: Kothari Satish Babu, Ponnuru Anil, Sahu Arabinda, Shimpi Nitin Ashok, Vellenki Siva Rama Prasad
Принадлежит: Mylan Laboratories Ltd.

The present invention relates to a novel process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol. 127.-. (canceled)30. The process according to or , wherein the step of separating the enantiomers and diasteromers of the compound of formula IV to obtain the compound of formula I is carried out via an enzymatic or a chemical process.32. The process according to claim 31 , wherein the catalyst used in step a) is N claim 31 ,N-dimethylamino pyridine.36. The process according to further comprising resolving or separating the enantiomers of the compound of formula IV to obtain the compound of formula I.3735. The process according to claim 35 , claim 35 , claim 35 , or claim 35 , wherein the compound of formula I is used as an intermediate in the preparation of HIV protease inhibitors.38. The process according to claim 37 , wherein the HIV protease inhibitor is Darunavir. This application claims priority to Indian patent application No 3518/CHE/2010 filed on Nov. 22, 2010 the contents of which are incorporated by reference in their entirety.The present invention relates to a process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol, which is useful as an intermediate in the preparation of protease ...

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Номер записи: 11
19-09-2013 дата публикации

Agrochemical Adjuvants and Formulations

Номер: US20130244877A1
Автор: Lindner Gregory James
Принадлежит: CRODA, INC.

Ethoxylated fatty acid mono-ester(s) of sorbitan with a fatty acid chain length from 8 to 14 and an overall degree of ethoxylation from 7 to 16 are new (though related to the polysorbates). These compounds are useful as adjuvants in agrochemical formulations, particularly combination formulations of herbicides having differing weed control effects, notably of non-selective herbicide and selective herbicide; particularly selective herbicide, particularly selective broadleaf herbicide, and graminicide; and selective graminicide and non-selective herbicide, especially a combination of a glyphosate type non-selective water soluble herbicide with a clethodim type selective (graminicide) herbicide, particularly to reduce or eliminate antagonism between differing types of herbicide. Formulations including such herbicide combinations and the adjuvant compounds are particularly useful in controlling weed including volunteer glyphosate resistant maize in subsequently sown glyphosate resistant soya. 1. A compound or mixture of compounds which is/are ethoxylated fatty acid mono-ester(s) of sorbitan in which the carbon chain length of the fatty acid is from 8 to 14 and the overall degree of ethoxylation is on average from 7 to 16.2. A compound or mixture of compounds according to claim 1 , where the ester(s) are compounds of formula (I):{'br': None, 'sub': n1', 'n2', 'n3', 'n4, 'sup': 1', '2', '3', '4, 'Sorb-(EOR)(EOR)(EOR)(EOR)\u2003\u2003(I)'} i) Sorb represents a residue obtained by removing four hydroxyl H atoms from sorbitan;', 'i) EO represents an ethyleneoxy residue;', 'ii) n1, n2, n3, and n4 each independently represent average values from 0 to 10;', 'iii) the total n1+n2+n3+n4 has an average value from 7 to 16; and', {'sup': 1', '2', '3', '4', '5', '5, 'sub': 7', '13, 'iv) R, R, R, and Reach independently represents H or an acyl group —C(O)—R, where Ris a Cto Chydrocarbyl.'}], 'wherein;'}3. A compound or mixture of compounds according to claim 2 , wherein an average of ...

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Номер записи: 12
10-10-2013 дата публикации

CONVERSION OF 5-(CHLOROMETHYL)-2-FURALDEHYDE INTO 5-METHYL-2-FUROIC ACID AND DERIVATIVES THEREOF

Номер: US20130267719A1
Автор: Cahana Aviad, Mikochik Peter
Принадлежит:

The present invention concerns the synthesis of 5-methyl-2-furoic acid, including ester, amide, and thioester derivatives of such from 5-(chloromethyl)-2-furaldehyde (CMF). The molecules so prepared are useful as intermediates for pharmaceutical, food, and fragrance molecules; as well as fuel or fuel additives. 1. A method for the synthesis of furan-containing molecules of formula I from furan-containing molecules of formula II , the method comprising: (a) contacting a furan-containing molecule of formula II , a base , an organic solvent , a catalyst , and a reactive nucleophile in a reaction vessel at a temperature of from about −78 degree C. to about 150 degree C. , such that furan-containing molecules of formula I are produced; (b) separating the product molecules of formula I by extraction with a hydrophobic solvent , or else by chromatography , distillation , sublimation , or precipitation.2. A method as in claim 1 , wherein R of formula I comprises oxygen claim 1 , sulfur claim 1 , and nitrogen.3. A method as in claim 1 , wherein R′ of formula I comprises carbon claim 1 , hydrogen claim 1 , sulfur claim 1 , nitrogen claim 1 , oxygen claim 1 , or any aromatic or aliphatic combination thereof;4. A method as in claim 1 , wherein R″ of formula II comprises chloride claim 1 , fluoride claim 1 , bromide claim 1 , iodide claim 1 , p-toluenesulfonate claim 1 , methanesulfonate claim 1 , trifluoroacetate claim 1 , phenoxy claim 1 , hydroxy claim 1 , or ammonium.5. A method as in claim 1 , wherein the base comprises an inorganic base.6. A method as in claim 1 , wherein the base comprises a nitrogen-containing organic base.7. A method as in claim 1 , wherein the organic solvent is miscible with water.8. A method as in claim 1 , wherein the organic solvent is immiscible with water.9. A method as in claim 1 , wherein the catalyst comprises nucleophilic anion groups consisting of cyanide claim 1 , chloride claim 1 , bromide claim 1 , or iodide.10. A method as in claim 1 , ...

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Номер записи: 13
14-11-2013 дата публикации

NOVEL 3,6-ANHYDRO-L-GALACTOSE DEHYDROGENASE ACTING ON 3,6-ANHYDRO-L-GALACTOSE, AND PRODUCTION OF 3,6-ANHYDROGALACTONIC ACID BY USING THE ENZYME

Номер: US20130303743A1
Автор: Choi In-Geol, Kim Kyoung Heon, LEE Saeyoung, YUN Eun Ju
Принадлежит: KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION

The present invention relates to a novel 3,6-anhydro-L-galactose dehydrogenase and to a novel compound produced therefrom. More specifically, provided is a 3,6-anhydro-L-galactose dehydrogenase which can produce 3,6-anhydrogalactonic acid of a novel type by metabolizing 3,6-anhydro-L-galactose. 1. 3 ,6-anhydro-L-galactose dehydrogenase having amino acid sequence as set forth in SEQ ID NOs: 1 to 4.2. A gene encoding 3 claim 1 ,6-anhydro-L-galactose dehydrogenase of .3. The gene of claim 2 , wherein the gene has sequences as set forth in SEQ ID NOs: 5 to 8.4. A recombinant vector containing the gene encoding 3 claim 2 ,6-anhydro-L-galactose dehydrogenase of .5. The recombinant vector of claim 4 , wherein the gene has sequences as set forth in SEQ ID NOs: 5 to 8.6. A transformant which is transformed with the recombinant vector of .7. A method of producing 3 claim 6 ,6-anhydro-L-galactose dehydrogenase which includes a step of obtaining 3 claim 6 ,6-anhydro-L-galactose dehydrogenase from a culture of the transformant of .9. The method of producing the compound of chemical formula 1 of claim 8 , wherein 3 claim 8 ,6-anhydro-L-galactose dehydrogenase has any one of amino acid sequences as set forth in SEQ ID NOs: 1 to 4.10. The method of producing the compound of the chemical formula 1 of claim 9 , wherein 3 claim 9 ,6-anhydro-L-galactose dehydrogenase is encoded by any one of sequences as set forth in SEQ ID NOs: 5 to 8. This application claims priority to and the benefit of Korean Patent Application No. 2011-0006631, filed Jan. 24, 2011, the disclosure of which is incorporated herein by reference in its entirety.1. Field of the InventionThe present invention relates to 3,6-anhydro-L-galactose dehydrogenase which produces a novel 3,6-anhydrogalatonic acid by metabolizing 3,6-anhydro-L-galactose as a bio energy production technology.2. Discussion of Related ArtThe world is currently facing depletion and rises in prices of petroleum resources, which are a major energy ...

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Номер записи: 14
21-11-2013 дата публикации

PROCESSES FOR PREPARING DIACIDS, DIALDEHYDES AND POLYMERS

Номер: US20130310578A1
Автор: Grushin Vladimir, Manzer Leo Ernest, Partenheimer Walter
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Alcohols are catalytically oxidized to aldehydes, in particular to benzaldehyde and diformylfuran, which are useful as intermediates for a multiplicity of purposes. The invention also relates to the polymerization of the dialdehyde and to the decarbonylation of the dialdehyde to furan. 1. A process for the preparation of a diacid of the formula HOOC—R′—COOH from an alcohol/aldehyde of the formula HOHC—R′—(C═O)H , wherein R′ is an optionally substituted furan ring , comprising the steps:{'sub': '2', '(a) contacting the alcohol/aldehyde with an oxidant in the presence of a metal bromide catalyst forming an alcohol/acid having the formula HOHC—R′—COOH, and optionally isolating the alcohol/acid;'}(b) contacting the alcohol/acid with an oxidant in the presence of a metal bromide catalyst forming an acid/aldehyde having the formula HOOC—R′—(C═O)H, and optionally isolating the acid/aldehyde;(c) contacting the acid/aldehyde with an oxidant in the presence of a metal bromide catalyst forming the diacid, optionally isolating the diacid.2. The process of claim1 wherein the product of the reaction is isolated following steps a , b or c.3. The process of wherein the process is run in a solvent or solvent mixture comprises at least one aliphatic C-Cmonocarboxylic acid solvent compound.4. The process of wherein the process is run in acetic acid.5. The process of wherein the metal bromide catalyst comprises a source of bromine and at least one metal selected from the group consisting of Co and Mn.6. The process of wherein the metal bromide catalyst further comprises Zr.7. The process of wherein the catalyst comprises Co and Mn.8. The process of wherein the process further comprises claim 4 , before step c claim 4 , converting the acid/aldehyde to an acetate ester of the formula CH(C═O)OCH—R′—(C═O)H.9. The process of wherein the diacid is furan-2 claim 8 ,5-dicarboxlic acid and the alcohol/aldehyde is 5-(hydroxymethyl)furfural. This application is a division of co-pending U.S. ...

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Номер записи: 15
28-11-2013 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

Номер: US20130317007A1
Автор: Anderson Eric, Jiang Xin, Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 34-. (canceled)710-. (canceled)11. The compound of claim 5 , wherein either Xor Xis OR claim 5 , wherein Ris absent.12. The compound of claim 6 , wherein Xis ORand Ris absent.13. The compound of claim 5 , wherein Xis hydrogen.14. (canceled)15. The compound of claim 6 , wherein Y is NRR.1617-. (canceled)18. The compound of claim 6 , wherein Ror Rcomprises a fluoro group.19. The compound of claim 18 , wherein one of Ror Rcomprises a trifluoromethyl group.20. The compound of claim 6 , wherein Rand Rare each independently hydrogen claim 6 , alkyl claim 6 , aryl claim 6 , aralkyl claim 6 , heteroaryl claim 6 , heteroaralkyl claim 6 , or a substituted version of any of these groups.2123-. (canceled)24. The compound of claim 6 , wherein Ris alkylsulfonyl claim 6 , arylsulfonyl claim 6 , aralkylsulfonyl claim 6 , heteroarylsulfonyl claim 6 , heteroaralkylsulfonyl claim 6 , or a substituted version of any of these groups.2529-. (canceled)30. The compound of claim 6 , wherein Ris acyl.31. The compound of claim 6 , wherein Ris substituted acyl.32. (canceled)33. The compound of claim 6 , wherein R′ is cyano.34. (canceled)35. The compound of claim 2 , wherein Ris absent.3637-. (canceled)38. The compound of claim 6 , wherein Rand Rare each methyl.39. The compound of claim 5 , wherein Rand Rare each hydrogen.40. The compound of claim 2 , wherein the bond joining carbon 1 and carbon 2 is a double bond.41. The compound of claim 6 , wherein the bond joining carbon 9 and carbon 11 is a double bond.42. The compound of claim 6 , wherein the bond joining carbon 9 and carbon 11 is a single bond.43. The compound of claim 5 , wherein the bond joining carbon 12 and carbon 13 is a single bond.44. The compound of claim 5 , wherein the bond joining carbon 13 and carbon 18 is a single bond.45. (canceled)47. (canceled)49. (canceled)51. (canceled)53. (canceled)55. (canceled)57. (canceled)59. ( ...

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Номер записи: 16
19-12-2013 дата публикации

C11 TO C13 DIALKYL ESTERS OF FURANDICARBOXYLIC ACID AS SOFTENERS

Номер: US20130338276A1
Автор: Becker Hinnerk Gordon, Grass Michael
Принадлежит: Evonik Oxeno GmbH

The invention relates to Cto Cdialkyl esters of furandicarboxylic acid. 1. A Cto Cdialkyl ester of furandicarboxylic acid.2. A plasticizer or plasticizer composition comprising the Cto Cdialkyl ester of .3. The plasticizer of claim 2 ,{'sub': 11', '13', '11', '13, 'wherein the Cto Cdialkyl ester is at least one Cto Cdialkyl furan-2,5-dicarboxylate.'}4. The plasticizer claim 2 ,{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'sub': 11', '13', '11', '13, 'of , wherein the Cto Cdialkyl ester is a mixture of at least two isomeric Cto Cdialkyl furan-2,5-dicarboxylates.'}5. The plasticizer of claim 4 ,wherein{'sub': 11', '13', '11', '13, 'the isomeric Cto Cdialkyl furan-2,5-dicarboxylates comprise isomeric Cto Calkyl groups.'}6. The plasticizer of claim 4 , wherein{'sub': 11', '13, 'none of the isomeric Cto Cdialkyl furan-2,5-dicarboxylates has a proportion of more than 90% by weight in the ester mixture.'}7. The plasticizer of claim 5 , wherein{'sub': 11', '13, 'the isomeric Cto Calkyl groups are at least one group selected from the group consisting of an unbranched alkyl group, a singly branched alkyl group, a doubly branched alkyl group, a triply branched alkyl group, and a quadruply branched alkyl group.'}8. The plasticizer of claim 2 , wherein the Cto Cdialkyl ester isditridecyl furan-2,5-dicarboxylate.9. The plasticizer{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'of , further comprising at least one additional compound selected from the group consisting of an alkyl benzoate, a dialkyl adipate, a glyceryl ester, a trialkyl citrate, an acylated trialkyl citrate, a trialkyl mellitate, a glycol dibenzoate, a dialkyl terephthalate, a dialkyl phthalate, a dialkanoyl ester of isosorbitol, and a dialkyl ester of 1,2-, 1,3- or 1,4-cyclohexanedicarboxylic acid.'}10. A process for preparing the plasticizer of claim 2 , the process comprising:{'sub': 11', '13, 'a) reacting a stoichiometric excess of one or more C-C-alcohols, optionally in the presence of a catalyst, ...

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Номер записи: 17
26-12-2013 дата публикации

METHOD FOR PREPARING A FURFURANOL-BASED COMPOUND AND 2-FURANCARBOXYLIC ACID-BASED COMPOUND USING AN IONIC LIQUID AS A SOLVENT

Номер: US20130345446A1
Автор: Chae Da Won, Cho Jin Ku, Kang Eun-Sil, Kim Baek Jin, Kim Sangyong, Kim Young Gyu
Принадлежит:

This invention relates to a method of, in an eco-friendly manner, preparing a furfuranol-based compound and a 2-furancarboxylic acid-based compound using an ionic liquid as a reaction solvent, which includes reacting a furfural-based compound with a hydroxide of an alkali metal or an alkaline earth metal using an ionic liquid as the solvent, thus obtaining a furfuranol-based compound and a 2-furancarboxylic acid-based compound, and in which water is not used as the reaction solvent, thus preventing the generation of reaction wastewater, and the ionic liquid used as the solvent can be easily recovered and reused. 2. The method of claim 1 , wherein Ris independently a valence bond or a Calkylene group claim 1 , and Ris independently a hydrogen atom or a Calkyl group.3. The method of claim 1 , further comprising claim 1 , after the reacting:adding a first organic solvent which selectively dissolves the ionic liquid and then performing filtering so that the furfuranol-based compound of Chemical Formula 2 and the 2-furancarboxylic acid-based compound in metal salt form of Chemical Formula 3 are filtered; andsubjecting the first organic solvent to fractional distillation to separate the ionic liquid from the first organic solvent which selectively dissolved the ionic liquid.4. The method of claim 3 , further comprising claim 3 , after the filtering:dissolving the furfuranol-based compound of Chemical Formula and the 2-furancarboxylic acid-based compound in metal salt form of Chemical Formula 3, which were filtered, in water to obtain a compound solution, adjusting a pH of the compound solution to 7˜8, adding a second organic solvent thereto, and then performing extraction, thus separating the furfuranol-based compound of Chemical Formula 2; andadjusting a pH of the solution from which the furfuranol-based compound of Chemical Formula 2 was extracted to an acidic range, adding a third organic solvent thereto, and then performing extraction, thus separating the 2- ...

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Номер записи: 18
26-12-2013 дата публикации

SEPARATING OFF 5 HYDROXYMETHYLFURFURAL (HMF) FROM REACTION SOLUTIONS BY STEAM DISTILLATION

Номер: US20130345450A1
Автор: Blank Benoit, Böhling Ralf, Feldner Carmen, Kindler Alois, Umlauf Sandra
Принадлежит: BASF SE

Method for producing solutions which comprise 5-hydroxymethylfurfural (HMF) and have a reduced content of starting materials of the HMF synthesis or a reduced content of by-products of the HMF synthesis (hereinbelow called product solution), which comprises treating solutions which comprise 114-. (canceled)16. The method of claim 15 , wherein the starting materials of the HMF synthesis are hexoses or oligomers or polymers composed of hexoses (hereinafter called saccharides).17. The method of claim 15 , wherein the by-products of the HMF synthesis are HMF oligomers.18. The method of claim 15 , wherein the polyether has a boiling point greater than 250° C. claim 15 , at standard pressure.19. The method of claim 15 , wherein the polyether is a poly-C2- to C4-alkylene glycol claim 15 , the terminal hydroxyl groups of which are optionally etherified with C1-C4 alkyl groups.20. The method of claim 15 , wherein the starting solution comprises the polyether in amounts of from 5% to 90% by weight.21. The method of claim 15 , wherein the starting solution is an aqueous solution.22. The method of claim 15 , wherein the treatment with steam takes place at 100° C. to 200° C.23. The method of claim 15 , wherein the treatment with steam takes place at a pressure of from 1 mbar to 300 mbar.24. The method of claim 15 , wherein the method is carried out continuously claim 15 , such that the starting solution and steam are fed to the evaporator continuously and the product solution is drawn off continuously.25. The method of claim 15 , wherein the evaporator is a thin-film evaporator.26. The method of claim 15 , wherein the steam is fed countercurrent to the starting solution.27. The method of claim 15 , wherein the percentage content of all saccharides in the product solution is in total less than 20% of the content of all saccharides in the starting solution.28. A process for producing 2 claim 15 ,5-furandicarboxylic acid or 2 claim 15 ,5-bis(hydroxymethyl)furan which comprises ...

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Номер записи: 19
26-12-2013 дата публикации

PROCESS FOR PURIFYING CRUDE FURAN 2,5-DICARBOXYLIC ACID USING HYDROGENATION

Номер: US20130345451A1
Автор: Janka Mesfin Ejerssa, Parker Kenny Randolph, Partin Lee Reynolds, Shaikh Ashfaq Schahanawaz
Принадлежит: EASTMAN CHEMICAL COMPANY

A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream is produced that is fed to a crystallization zone followed by a solid-liquid displacement zone to form a low impurity slurry stream. The solids in the low impurity slurry stream are dissolved in a dissolution zone to produce a hydrogenation feed that is hydrogenated in a hydrogenation reactor to generate a hydrogenated FDCA composition. The hydrogenated FDCA composition is routed to a crystallization zone to form a crystallized produce stream that is separated from liquid in a solid-liquid separation zone to generate a purified wet cake stream containing FDCA that can be dried in a drying zone to generate a dry purified FDCA product stream. 1. A process for purifying a crude furan 2 ,5-dicarboxylic acid composition (cFDCA) comprising:a) providing a cFDCA composition comprising furan 2,5-dicarboxylic acid (FDCA) solids, 5-formyl furan-2-carboxylic acid (FFCA), and a liquid oxidation solvent composition;b) separating at least a portion of the oxidation solvent from the FDCA solids in the cFDCA composition in a first solid-liquid separation zone to generate a concentrated cFDCA composition comprising FDCA solids and enriched in the concentration of solids relative to the concentration of solids in the cFDCA composition fed to the first solid-liquid separation zone;c) feeding the concentrated cFDCA composition to a dissolution zone in which a hydrogenation solvent composition is combined with the FDCA solids in the concentrated cFDCA composition and dissolving at least a portion of said FDCA solids to thereby produce a solvated FDCA composition (sFDCA) comprising dissolved furan 2,5-dicarboxylic acid (FDCA), a hydrogenation solvent, and 5-formyl furan-2-carboxylc acid (FFCA);d) subjecting the sFDCA composition to a hydrogenation reaction in a hydrogenation reaction zone under conditions sufficient to cause ...

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Номер записи: 20
26-12-2013 дата публикации

PURIFYING CRUDE FURAN 2,5-DICARBOXYLIC ACID BY HYDROGENATION

Номер: US20130345452A1
Автор: Janka Mesfin Ejerssa, JR. Charles Edwan, Kirk Shane Kipley, Parker Kenny Randolph, Shaikh Ashfaq Shahanawaz, Sumner
Принадлежит: EASTMAN CHEMICAL COMPANY

A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA). 1. A process for purifying a crude furan 2 ,5-dicarboxylic acid composition (cFDCA) comprising:a) providing a cFDCA composition comprising furan 2,5-dicarboxylic acid (FDCA) solids, 5-formyl furan-2-carboxylc acid (FFCA), and a oxidation solvent composition;b) combining a hydrogenation solvent composition with said FDCA solids and dissolving at least a portion of the FDCA solids to thereby produce a solvated FDCA (sFDCA) composition comprising dissolved FDCA, the hydrogenation solvent composition, and FFCA;c) in a hydrogenation reaction zone, hydrogenating the sFDCA at a temperature within a range of 130° C. to 225° C. by contacting the sFDCA composition with hydrogen in the presence of a hydrogenation catalyst to thereby hydrogenate FFCA and produce a furan 2,5-dicarboxylic acid composition (hFDCA) comprising a hydrogenated FFCA species, dissolved FDCA, and said hydrogenation solvent; ande) separating at least a portion of the dissolved FDCA from the hFDCA composition to obtain a product FDCA (pFDCA) composition.2. The process of claim 1 , wherein the cFDCA composition comprises at least 15 wt. % solids based on the weight of the cFDCA composition claim 1 , wherein at least 85 wt. % of the solids is FDCA based on the weight of the solids; and FFCA.3. The process of claim 2 , wherein the cFDCA composition comprises at least 28 wt. % solids based on the weight of ...

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Номер записи: 21
26-12-2013 дата публикации

PROCESS FOR THE DEPOLYMERIZATION OF A FURANDICARBOXYLATE CONTAINING POLYESTER

Номер: US20130345453A1
Автор: Olson Michael Leroy, Sipos Laszlo
Принадлежит: FURANIX TECHNOLOGIES B.V.

A product including a furandicarboxylate compound and diol is obtained from a furandicarboxylate containing polyester in a process, which includes reacting a polymer composition including furandicarboxylate containing polyester with water or an alcohol, such as an alkyl alcohol with from 1 to 12 carbon atoms, in the presence of a base, that is preferably selected from the group consisting of metal hydrides, metal alkoxides, metal carbonates, metal carboxylates, N-heterocyclic carbenes, amidines, guanidines, phosphazenes and mixtures thereof. 1. A process for the depolymerization of a furandicarboxylate containing polyester , which process comprises reacting the polyester with an alcohol or water in the presence of a depolymerisation catalyst to yield a product comprising a furandicarboxylate compound and diol.2. The process according to claim 1 , wherein the polyester comprises poly(alkylene 2 claim 1 ,5-furandicarboxylate).3. The process according to claim 2 , wherein the alkylene moiety of the poly(alkylene 2 claim 2 ,5-furandicarboxylate) comprises 2 to 6 carbon atoms.4. The process according to any claim 1 , wherein the depolymerisation catalyst comprises an acid catalyst claim 1 , a metal compound or a base.5. The process according to claim 4 , wherein the depolymerisation catalyst comprises a base.6. The process according to claim 5 , wherein the base is selected from the group consisting of metal alkoxides claim 5 , metal hydroxides claim 5 , metal carbonates claim 5 , metal carboxylates claim 5 , N-heterocyclic carbenes claim 5 , amidines claim 5 , guanidines claim 5 , phosphazenes and mixtures thereof.7. The process according to claim 1 , which is preceded by dispersing at least part of the polyester in an alcohol or water to yield a polyester slurry.8. The process according to claim 1 , where claim 1 , when water and a base are used claim 1 , free dicarboxylic acid is obtained after treatment with a Brønsted acid.9. The process according to claim 1 , ...

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Номер записи: 22
09-01-2014 дата публикации

CONVERSION OF BIOMASS

Номер: US20140011248A1
Автор: Cooper Christopher, Khan Jihan, Masterman Thomas Craig, Medoff Marshall
Принадлежит:

Biomass feedstocks (e.g., plant biomass, animal biomass, and municipal waste biomass) are processed to produce useful products, such as fuels. For example, systems are described that can convert feedstock materials to a sugar solution, especially, xylose, which can then be chemically converted to furfural and furfural-derived products. 1. A method for converting a sugar , the method comprising;converting xylose to a product or an intermediate, the xylose being obtained by treating biomass with irradiation and saccharification.2. The method of wherein converting comprises chemically converting the xylose to the product or the intermediate.3. The method of wherein converting comprises reacting the xylose using reactions selected from the group consisting of cyclization reactions claim 2 , polymerization reactions claim 2 , condensation reactions claim 2 , reduction reactions claim 2 , oxidation reactions claim 2 , esterification reactions claim 2 , alkylation reactions claim 2 , decarbonylation claim 2 , and combinations thereof.4. The method of wherein the product or intermediate comprises furfural.5. The method wherein converting further comprises reacting the xylose or the intermediate over an acid catalyst.6. The method of wherein the acid catalyst is selected from the group consisting of acidified Zeolites claim 5 , acidified silica claim 5 , surface grafted silicas claim 5 , functionalized mesoporous silicas claim 5 , poly acids claim 5 , acid functionalized polymers claim 5 , poly sulfonic acids claim 5 , poly acetic acids claim 5 , poly phosphonic acids claim 5 , polystyrene sulfonic acids claim 5 , tetraorthosilicates claim 5 , 3-(mercaptopropyl)trimethoxysilane claim 5 , Lewis acids claim 5 , microporous silicoaluminophosphate claim 5 , metal oxides claim 5 , ZrO claim 5 , AlO claim 5 , TiO claim 5 , SiO claim 5 , V203 claim 5 , sulfate salts claim 5 , (NH)SOmetal halides claim 5 , MgC claim 5 , LaC claim 5 , FeCl claim 5 , metal carbonates claim 5 , CsCO ...

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Номер записи: 23
23-01-2014 дата публикации

SULFONAMIDE DERIVATIVE AND USE THEREOF

Номер: US20140024650A1
Автор: ASANO Yasutomi, Fukuda Koichiro, Fukumoto Shoji, IMAEDA Toshihiro, Iwanaga Kouichi, KORI Masakuni, Mikami Satoshi, Morimoto Shinji, Nakamura Shinji, Tokunaga Norihito, Ujikawa Osamu
Принадлежит: Takeda Pharmaceutical Company Limited

Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): 2. The compound according to claim 1 , wherein ring A is{'sub': '3-6', 'optionally further substituted Ccycloalkane,'}an optionally further substituted tetrahydrofuran ring,an optionally further substituted tetrahydropyran ring,an optionally further substituted piperidine ring,an optionally further substituted tetrahydrothiopyran ring oran optionally further substituted 8-oxabicyclo[3.2.1]octane ring,or a salt thereof.3. The compound according to claim 1 , wherein the substituent(s) on the ring A is(are) selected from(1) 1 to 3 halogen atoms,{'sub': '1-6', '(2) a Calkyl group optionally substituted by one phenyl group,'}{'sub': '1-6', '(3) a carbamoyl group substituted by a Calkyl group,'}{'sub': '1-6', '(4) a Calkyl-carbonyl group,'}{'sub': '1-6', '(5) a Calkoxy-carbonyl group,'}(6) an oxo group,(7) a hydroxyl group and{'sub': '1-6', '(8) a Calkylsulfonyl group,'}or a salt thereof.5. The compound according to claim 1 , wherein ring B is a benzene ring claim 1 , or a salt thereof.6. The compound according to claim 1 , wherein the substituent on the ring B is selected from(1) a halogen atom;(2) a cyano group;{'sub': '1-6', '(3) a Calkyl group optionally substituted by 1 to 3 substituents selected from a halogen atom and a cyano group;'}{'sub': '1-6', '(4) a hydroxyl group optionally substituted by a Calkyl group optionally substituted by 1 to 3 halogen atoms or a phenyl group (including alkoxy);'}{'sub': 1-6', '1-6, '(5) an amino group optionally substituted by 1 or 2 substituents selected from a Calkyl group, a Calkyl-carbonyl and a phenyl group;'}{'sub': '3-6', '(6) a Ccycloalkyl group;'}(7) a tricyclo[3.3.1.1.3.7]decyl group;(8) phenyl optionally substituted by 1 to 3 substituents selected ...

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Номер записи: 24
06-02-2014 дата публикации

Squarylated Lactones Inhibitors for Bacterial Biofilm Formation

Номер: US20140039195A1
Автор: FALCONE Eric, Luk Yan-Yeung, Narasimhan Sri Kamesh
Принадлежит: SYRACUSE UNIVERSITY

A library of unnatural squarylated homoserine lactones (SHLs) and squarylated lactones that bear potential to modulate biofilm formation in Gram negative bacteria. At low concentrations (˜200 μM), these small molecules inhibit biofilm formation of . Moreover, these compounds are not toxic up to 300 μM and do not significantly attenuate growth. The SHLs have potential to disperse established biofilm and demonstrate an enhanced reduction (˜50%) of the maximum biofilm thickness by use of SHLs during biofilm growth. 2. The squarylated homoserine lactone of claim 1 , wherein said squarylated homoserine lactone is characterized by an ability to modulate quorum sensing.3. The squarylated homoserine lactone of claim 1 , wherein said squarylated homoserine lactone is characterized by an ability to inhibit biofilms.6. The squarylated homoserine lactone of claim 5 , wherein said squarylated homoserine lactone is characterized by an ability to modulate quorum sensing.7. The squarylated homoserine lactone of claim 5 , wherein said squarylated homoserine lactone is characterized by an ability to inhibit biofilms.8. A method of producing a squarylated homoserine lactone claim 5 , comprising the steps of:(a) subjecting 3,4-dibutoxy-cyclobut-3-ene-1,2-dione to Grignard/organolithium reagents to produce a 1,2 addition reaction; and(b) treating the product of step (a) with trifluoroacetic anhydride;(c) performing hydrolysis of the product of step (b) to produce a squarylated ester intermediate; and(d) treating said squarylated ester intermediate with and α-Amino-γ-butyrolactone to produce a squarylated homoserine lactone.10. The method of claim 9 , wherein said squarylated homoserine lactone is characterized by an ability to modulate quorum sensing.11. The method of claim 9 , wherein said squarylated homoserine lactone is characterized by an ability to inhibit biofilms.14. The method of claim 8 , wherein said squarylated homoserine lactone is characterized by an ability to modulate ...

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Номер записи: 25
06-02-2014 дата публикации

PROCESS FOR CONVERTING POLYSACCHARIDES IN AN INORGANIC MOLTEN SALT HYDRATE

Номер: US20140039208A1
Автор: "OConnor Paul", MAKKEE Michiel, MENEGASSI DE ALMEIDA Rafael, Moulijn Jacob Adriaan
Принадлежит: BIOECON INTERNATIONAL HOLDING N.V.

A process is disclosed for converting polysaccharides to platform chemicals. The process comprises dissolving the polysaccharides in a inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to platform chemicals that are easily separable from the inorganic molten salt hydrate. 128.-. (canceled)29. A process for converting ligno-cellulosic biomass to platform chemicals , said process comprising the steps of:a) dissolving ligno-cellulosic biomass in an inorganic molten salt hydrate;b) converting the dissolved ligno-cellulosic biomass to monosaccharides;c) converting the monosaccharides to platform chemicals that are easily separable from the inorganic molten salt hydrate;d) separating the platform chemicals from the inorganic molten salt hydrate.30. The process of claim 29 , further comprising: pre-treating the lignocellulosic biomass through comminution claim 29 , or subjecting the ligno-cellulosic biomass to comminution during step a).31. The process of claim 29 , wherein the molten salt hydrate comprises a composition claim 29 , the composition comprising at least Zn claim 29 , Ca or Li halides claim 29 , or mixtures thereof claim 29 , with a content of 40 to 80 wt % of salt in said composition.32. The process of claim 29 , wherein in step b) claim 29 , the acid is an inorganic soluble acid.33. The process of claim 29 , wherein lignin is separated out after step b).34. The process of claim 29 , wherein acid is removed prior to step c).35. The process of claim 29 , wherein step c) takes place in a fixed bed catalyst claim 29 , slurry reactor claim 29 , expanded bed catalyst claim 29 , moving bed catalyst claim 29 , or trickle bed catalyst.36. The process of claim 29 , wherein the hydrogenation catalyst is selected from a noble metal of the series of Ru claim 29 , Rh claim 29 , Pd and Pt claim 29 , or a transition metal of the series Cu claim 29 , Cr claim 29 , Co claim 29 , Ni and Fe.37. The process of ...

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Номер записи: 26
13-02-2014 дата публикации

METHODS AND COMPOSITIONS FOR TREATING METABOLIC SYNDROME

Номер: US20140045933A1
Автор: Kalayoglu Murat V.
Принадлежит: Terakine Therapeutics, Inc.

Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein, L, R; R, Z, X, A and B are defined herein. 3. The method of claim 1 , wherein the disorder associated with metabolic syndrome is obesity.4. The method of where the method reduces adipocytes in the subject.5. The method of wherein the disorder associated with metabolic syndrome is dyslipidemia.6. The method of claim 5 , wherein the method reduces triglycerides claim 5 , reduces LDL claim 5 , reduces total cholesterol claim 5 , and/or increases HDL in the subject.7. The method of wherein the disorder associated with metabolic syndrome is a diabetic condition.8. The method of claim 7 , wherein the diabetic condition is type 2 diabetes mellitus.9. The method of claim 8 , wherein the method reduces serum glucose claim 8 , reduces glycated hemoglobin claim 8 , reduces serum insulin claim 8 , improves glucose tolerance claim 8 , reduces the subject's need for insulin claim 8 , and/or reduces the incidence of a diabetic complication in the subject.10. The method of claim 1 , wherein the subject suffers from or is likely to suffer from a disease claim 1 , disorder or condition selected from the group consisting of metabolic syndrome claim 1 , overweight claim 1 , obesity claim 1 , dyslipidemia claim 1 , hypercholesterolemia claim 1 , hypertriglyceridemia claim 1 , diabetes mellitus claim 1 , vascular disease claim 1 , atherosclerosis claim 1 , coronary artery disease claim 1 , stroke claim 1 , cerebrovascular disease claim 1 , peripheral vascular disease claim 1 , fatty liver claim 1 , pancreatitis claim 1 , inflammation or ...

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Номер записи: 27
20-02-2014 дата публикации

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Номер: US20140051867A1
Автор: EVANS Jared Wayne, Fujimori Shinji, Huynh Grace M., Liu Qi, Teresk Martin Gerald
Принадлежит: Gilead Sciences, Inc.

The present disclosure provides processes for the preparation of a compound of Formula I: 5. The process of claim 3 , wherein the N-arylation reaction conditions comprise a catalyst.6. The process of claim 5 , wherein the catalyst is a palladium claim 5 , platinum claim 5 , or copper based catalyst.7. The process of claim 6 , wherein the catalyst is selected from the group consisting of tris(dibenzylideneacetone)dipalladium(0) claim 6 , copper(I) chloride claim 6 , copper(II) chloride claim 6 , copper(I) bromide claim 6 , copper(II) bromide claim 6 , copper(I) acetate claim 6 , copper(II) acetate claim 6 , copper(II) acetylacetonate claim 6 , copper(I) trifluoromethanesulfonate claim 6 , copper(II) trifluoromethanesulfonate claim 6 , copper(I) thiophene-2-carboxylate claim 6 , and copper(I) iodide.8. The process of claim 3 , wherein the N-arylation reaction conditions further comprise a ligand.9. The process of claim 8 , wherein the ligand is selected from the group consisting of 5-(di-tert-butylphosphino)-1′ claim 8 ,3′ claim 8 ,5′-triphenyl-1′H-[1 claim 8 ,4]bipyrazole claim 8 , 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole claim 8 , 2-(di-tert-butylphosphino)-1-(2-methoxyphenyl)-1H-pyrrole claim 8 , acetylacetone claim 8 , acetylcyclohexanone claim 8 , isobutyrylcyclohexanone claim 8 , N claim 8 ,N-dimethylcyclohexane-1 claim 8 ,2-diamine claim 8 , L-proline claim 8 , BINAP claim 8 , and N claim 8 ,N-diethylsalicylamide.10. The process of claim 3 , wherein the N-arylation reaction conditions comprise a base.11. The process of claim 10 , wherein the base is selected from the group consisting of potassium hydroxide claim 10 , sodium hydroxide claim 10 , sodium tert-amylate claim 10 , cesium carbonate claim 10 , cesium hydroxide claim 10 , potassium phosphate tribasic claim 10 , sodium tertbutoxide claim 10 , sodium methoxide claim 10 , and sodium ethoxide.12. The process of claim 3 , wherein the N-arylation reaction conditions comprise a phase transfer catalyst. ...

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Номер записи: 28
27-02-2014 дата публикации

TRI-SUBSTITUTED 2-BENZHYDRYL-5-BENZYLAMINO-TETRAHYDRO-PYRAN-4-OL AND 6-BENZHYDRYL-4-BENZYLAMINO-TETRAHYDRO-PYRAN-3-OL ANALOGUES, AND NOVEL 3,6-DISUBSTITUTED PYRAN DERIVATIVES

Номер: US20140058120A1
Автор: DUTTA Aloke K.
Принадлежит: WAYNE STATE UNIVERSITY

Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants. 124-. (canceled) This application is a continuation of U.S. Ser. No. 12/836,878, filed Jul. 15, 2010, issued as U.S. Pat. No. 8,519,159 on Aug. 27, 2013, which is a continuation of U.S. Ser. No. 10/599,892, filed Oct. 12, 2006, issued as U.S. Pat. No. 7,915,433 on Mar. 29, 2011, which is a national phase of PCT/US05/12748, filed Apr. 15, 2005, which claims the benefit of U.S. provisional application Ser. No. 60/563,189, filed Apr. 16, 2004, the entire disclosures of each of which are hereby incorporated by reference herein.1. Field of the InventionThe invention pertains to pharmacologically active 3,6-disubstituted pyran compounds and similar compounds having additional substitution on the pyran ring. The compounds show high activity at monoamine transporters, and thus can be used to alter reuptake of monoamines in treatment of numerous diseases in mammalian species for which alteration of the monoamine transport system is indicated.2. Background ArtThe monoamine transporters terminate the action of released biogenic amines such as dopamine (DA), norepinephrine (NE) and serotonin (5-HT) in the central nervous system (CNS) and are known as dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter (SERT), respectively.These transporters play a vital role in maintaining the extracellular concentration of biogenic amine neurotransmitters.Drugs binding to the DAT are typically regarded as stimulants. Cocaine- and amphetamine-related compounds are known to produce their action by binding to both DAT and SERT with cocaine acting as a blocker and amphetamine as a substrate.On the other hand, drugs binding to the SERT and NET are known to produce, among other effects, potent antidepressant activity.Major depression disorder is a significant health problem, and behind cardiovascular ...

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Номер записи: 29
06-03-2014 дата публикации

OXIDATION PROCESS TO PRODUCE A CRUDE DRY CARBOXYLIC ACID PRODUCT

Номер: US20140066639A1
Автор: Janka Mesfin Ejerssa, Parker Kenny Randolph, Partin Lee Reynolds, Shaikh Ashfaq Shahanawaz
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH-furfural where R=alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R′OCH-furfural, where R′=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R″-furfural, where R″=alkyl, cycloalkyl and aryl), mixed feed-stocks of 5-HMF and 5-HMF esters and mixed feed-stocks of 5-HMF and 5-HMF ethers and mixed feed-stocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA, cooling a crude carboxylic acid slurry in cooling zone to form a cooled slurry stream. The cooled slurry stream is routed to a solid-liquid separation zone to generate a crude wet cake stream comprising FDCA that is dried in a drying zone to generate a dry carboxylic acid product stream comprising crude FDCA (cFDCA). 1. A process to produce a carboxylic acid composition , said process comprising:{'sub': 2', '2, '(a) oxidizing in an primary oxidation zone an oxidizable compound in a oxidizable raw material stream in the presence of a solvent stream, an oxidizing gas stream, and a catalyst system, wherein said an oxidizable raw material stream comprises at least one compound selected from the group consisting of 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH-furfural where R=alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R′OCH-furfural, where R′=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R″-furfural, where R″=alkyl, cycloalkyl and aryl), mixed feedstocks of 5-HMF and 5-HMF esters, mixed feedstocks of 5-HMF and 5-HMF ethers, and mixed feedstocks of 5-HMF and 5-alkyl furfurals to produce a carboxylic acid composition comprising furan-2,5-dicarboxylic acid (FDCA);'}(b) routing said carboxylic acid composition to a cooling zone;(c) routing cooled carboxylic acid composition to a solid-liquid ...

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Номер записи: 30
13-03-2014 дата публикации

PROCESS FOR MANUFACTURING ESTERS OF 2,5-FURANDICARBOXYLIC ACID

Номер: US20140073805A1
Автор: Franke Oliver, Richter Oliver
Принадлежит: Clariant Produkte (Deutschland) GmbH

The present invention relates to an improved process for manufacturing of esters of 2,5-furandicarboxylic acid (FD-CA-esters) by reacting 2,5-furandicarboxylic acid (FDCA) with one or more alcohols in the presence of a heterogeneous catalyst. The use of the heterogeneous catalyst, which may be a Bronsted or Lewis acid, allows for production of high yields of FDCA esters. Furthermore, the catalyst can conveniently be recycled after completion of the reaction. 1. A process for manufacturing esters of 2 ,5-furandicarboxylic acid by comprising reacting 2 ,5-furandicarboxylic acid with one or more alcohols in the presence of a heterogeneous catalyst.2. The process according to claim 1 , wherein the catalyst is a Bronsted and/or Lewis acid catalyst.3. The process according to claim 1 , wherein the heterogeneous catalyst is selected from the group consisting ofa) silica-based materialsb) claysc) aluminasd) ion exchange resinse) metal oxidesf) heteropoly acidsg) hydroxyapatite.4. The process according to claim 3 , wherein the heterogeneous catalyst is a silica-based material selected from the group consisting ofa1) amorphous silica-aluminasa2) zeolitesa3) mesoporous molecular sieves.5. The process according to claim 4 , wherein the catalyst is amorphous silica-alumina claim 4 , preferably with an AlO/SiOratio from 0.2 to 20 claim 4 , more preferably with an AlO/SiOratio from 1.0 to 3.0 claim 4 , and most preferably with an AlO/SiOratio from 2.0 to 2.5.6. The process according to claim 4 , wherein the heterogeneous catalyst is a zeolite claim 4 , preferably of the type FAU claim 4 , MOR claim 4 , MFI claim 4 , LTA or BEA claim 4 , and especially preferred of the type FAU with an SiO/AlOratio from 2 to 100.7. The process according to claim 4 , wherein the heterogeneous catalyst is a mesoporous molecular sieve claim 4 , preferably a metal-doped mesoporous molecular sieve claim 4 , and more preferably an aluminium-doped mesoporous molecular sieve type MCM-41 with a Si/Al ratio ...

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Номер записи: 31
20-03-2014 дата публикации

HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE

Номер: US20140080790A1
Автор: IKEHARA OSAMU, KODAMA Yuko, KONISHI Atsushi, Koshiba Takahiro, Ohsumi Koji, Suzuki Tamotsu, Tokumasu Munetaka
Принадлежит: AJINOMOTO CO., INC.

Compounds represented by formula (I): 122-. (canceled)25. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a halogeno group.27. A method according to claim 23 , wherein X is a lower alkylene group optionally having substituent(s) or a lower alkenylene group optionally having substituent(s) claim 23 , wherein said substituent(s) is selected from the group consisting of a halogeno group claim 23 , a hydroxyl group claim 23 , an amino group claim 23 , a lower alkyl group claim 23 , a lower alkoxyl group claim 23 , and a lower acyl group.28. A method according to claim 23 , wherein Y is a carbonyl group or a sulfonyl group.30. A method according to claim 29 , wherein R60 is a carboxyl group claim 29 , a sulfo group claim 29 , a lower alkoxycarbonyl group claim 29 , or a hydroxyl group claim 29 ,D is a lower alkylene group optionally having substituent(s), wherein said substituent(s) is selected from the group consisting of a halogeno group, a hydroxyl group, a thiol group, an amino group, a guanidino group, a carboxyl group, a sulfo group, a lower alkoxyl group, a lower alkylthio group, a lower alkylamino group, a lower acylamino group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkylsulfonylamino group, an arylsulfonylamino group optionally having substituent(s), an aryl group optionally having substituent(s), a heterocyclic group optionally having substituent(s), and an oxo group, andR70 is a hydrogen atom, a hydroxyl group, a lower alkyl group optionally having substituent(s), or a lower alkoxyl group optionally having substituent(s),or R70 and D may be bonded to form a cyclic amino group optionally having substituent(s).31. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a fluorine atom ...

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Номер записи: 32
04-01-2018 дата публикации

Hypdh inhibitors and methods of use for the treatment of kidney stones

Номер: US20180002275A1
Автор: Daniel Yohannes, Ross P. Holmes, W. Todd Lowther
Принадлежит: UAB RESEARCH FOUNDATION, Wake Forest University Health Sciences

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).

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Номер записи: 33
05-01-2017 дата публикации

METHODS AND COMPOUNDS FOR PRODUCING NYLON 12

Номер: US20170002142A1
Автор: Klein Josef Peter
Принадлежит: EMPIRE TECHNOLOGY DEVELOPMENT LLC

Nylon 12 may be produced by dimerization of 6-carbon furan compounds into 12-carbon dimers, and conversion of the dimers into nylon 12. The 6-carbon furan compounds may be produced from biomass. Ester-aldehyde dimers and amino-ester dimers may be produced from the 6-carbon furan compounds as precursors for at least the production of nylon 12, and the components for producing the nylon 12 may be provided as a kit. 2. (canceled)3. The method of claim 1 , wherein converting the amino-ester to nylon 12 comprises treating the amino-ester with a halide source and hydrogen gas in a presence of a catalyst.5. (canceled)6. The method of claim 3 , wherein is treating the amino-ester comprises treating with hydrogen iodide claim 3 , hydrogen chloride claim 3 , hydrogen bromide claim 3 , or any combination thereof in a presence of a catalyst including platinum claim 3 , palladium claim 3 , rhodium claim 3 , ruthenium claim 3 , nickel claim 3 , cobalt claim 3 , iron claim 3 , molybdenum claim 3 , iridium claim 3 , rhenium claim 3 , gold claim 3 , or any combination thereof.79-. (canceled)10. The method of claim 1 , further comprising producing the alkyl furan compounds including 5-chloromethylfurfural by isolating hexoses claim 1 , sucrose claim 1 , cellulose claim 1 , corn stover claim 1 , or any combination thereof from biomass and heating the hexoses claim 1 , sucrose claim 1 , cellulose claim 1 , corn stover claim 1 , or any combination thereof in a presence of one or more of 1 claim 1 ,2-dichloroethane claim 1 , an acid claim 1 , and an alkaline salt.11. (canceled)12. The method of claim 10 , wherein heating includes heating in a presence of lithium halide claim 10 , sodium halide claim 10 , potassium halide claim 10 , or any combination thereof.13. (canceled)15. The method of claim 14 , wherein converting the 5-chloromethyl furan compounds to the dimethylacetal protected Wittig reagent comprises treating the 5-chloromethyl furan compounds with triphenylphosphine claim 14 , ...

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Номер записи: 34
02-01-2020 дата публикации

PALLADIUM-MEDIATED KETOLIZATION

Номер: US20200002352A1
Автор: Kishi Yoshito, LEE Jung Hwa, Li Zhanjie, Osawa Ayumi
Принадлежит: President and Fellows of Harvard College

Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer). 1111-. (canceled)114144-. (canceled)146. The compound of claim 112 , wherein Ris optionally substituted Calkyl.147. The compound of claim 146 , wherein Ris unsubstituted Calkyl.148. The compound of claim 146 , wherein Ris methyl.150153-. (canceled)154. The compound of claim 112 , wherein Ris hydrogen.155. The compound of claim 112 , wherein Ris hydrogen.156159-. (canceled)160. The compound of claim 112 , wherein Rand Rare hydrogen.161. The compound of claim 112 , wherein R claim 112 , R claim 112 , and Rare optionally substituted Calkyl.162. The compound of claim 161 , wherein R claim 161 , R claim 161 , and Rare unsubstituted Calkyl.163. The compound of claim 161 , wherein R claim 161 , R claim 161 , and Rare methyl.164. (canceled)165. A pharmaceutical composition comprising a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 , and optionally a pharmaceutically acceptable excipient.166. A method of inhibiting mitosis in a subject in need thereof claim 112 , the method comprising administering to the subject a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 , or a pharmaceutical composition thereof claim 112 , in an amount sufficient to inhibit mitosis.167. A method of triggering apoptosis in cell of a subject claim 112 , the method comprising administering to the subject a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 ...

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Номер записи: 35
04-01-2018 дата публикации

MACROCYCLIZATION REACTIONS AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF ANALOGS OF HALICHONDRIN B

Номер: US20180002342A1
Автор: Chase Charles E., CHOI Hyeong-Wook, Fang Francis G., Kim Dae-Shik, LEE Jaemoon
Принадлежит:

The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same. 1. A method of preparing an intermediate in the synthesis of eribulin , said method comprising performing a macrocyclization reaction on a non-macrocyclic intermediate , said macrocyclization reaction producing said intermediate in the synthesis of eribulin by forming C.15-C.16 , C.2-C.3 , C.3-C.4 , C.19-C.20 , C.0-C.1 , or C.26-C.27 bond in the structure of eribulin.2. The method of claim 1 , wherein said performing said macrocyclization reaction comprises contacting said non-macrocyclic intermediate with an olefin metathesis catalyst.4. The method of claim 3 , wherein each Pand Pis independently a hydroxyl protecting group.5. The method of or claim 3 , wherein at least one of Pand Pis a hydroxyl protecting group.6. The method of any one of to claim 3 , wherein Rand Rcombine to form a bond claim 3 , and Ris H.7. The method of any one of to claim 3 , wherein Rand Rcombine to form a bond claim 3 , and Ris H.8. The method of claim 1 , wherein said performing said macrocyclization reaction comprises contacting said non-macrocyclic intermediate with an organic base and a Lewis acid.10. The method of claim 9 , wherein each R is optionally substituted Calkyl.11. The method of or claim 9 , wherein at least one of Pand Pis a hydroxyl protecting group.12. The method of any one of to claim ...

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Номер записи: 36
07-01-2021 дата публикации

METHOD FOR PURIFYING CRUDE 2,5-FURANDICARBOXYLIC ACID COMPOSITION

Номер: US20210002243A1
Автор: Liu Shu-Wei, Lu Xin-An
Принадлежит: FAR EASTERN NEW CENTURY CORPORATION

A method for purifying a crude 2,5-furandicarboxylic acid composition including 2,5-furandicarboxylic acid and 2-furoic acid is disclosed. The method includes the steps of: (a) mixing the crude 2,5-furandicarboxylic acid composition with a solvent solution that includes alcohol so as to obtain a mixture; (b) heating the mixture to permit full dissolution of the crude 2,5-furandicarboxylic acid composition in the solvent solution; and (c) cooling the mixture to permit recrystallization of the 2,5-furandicarboxylic acid from the mixture so as to obtain purified 2,5-furandicarboxylic acid. 1. A method for purifying a crude 2 ,5-furandicarboxylic acid composition , which includes 2 ,5-furandicarboxylic acid and 2 furoic acid , the method comprising the steps of:(a) mixing the crude 2,5-furandicarboxylic acid composition with a solvent solution that includes alcohol and water present in a weight ratio ranging from 5:1 to 5:5 to obtain a mixture;(b) heating the mixture to permit full dissolution of the crude 2,5-furandicarboxylic acid composition in the solvent solution; and(c) cooling the mixture to permit recrystallization of the 2,5-furandicarboxylic acid from the mixture, so as to obtain purified 2,5-furandicarboxylic acid.2. The method as claimed in claim 1 , wherein the alcohol is selected from the group consisting of methanol claim 1 , ethanol claim 1 , isopropanol claim 1 , and combinations thereof.3. (canceled)4. (canceled)5. The method as claimed in claim 1 , wherein in step (b) claim 1 , the mixture is heated to a first temperature ranging from 40° C. to 120° C.6. The method as claimed in claim 1 , wherein in step (c) claim 1 , the mixture is cooled to a second temperature ranging from 0° C. to 30° C.7. The method as claimed in claim 1 , wherein step (c) includes:recrystallizing the 2,5-furandicarboxylic acid from the mixture; andseparating the 2-furoic acid in the mixture from the 2,5-furandicarboxylic acid.8. The method as claimed in claim 7 , wherein ...

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Номер записи: 37
20-01-2022 дата публикации

NONIONIC POLYETHER SURFACTANTS

Номер: US20220017480A1
Автор: Baraznenok Ivan, GALL Alexander A.
Принадлежит: Cepheid

Non-ionic polyether surfactants with improved resistance to hydrolysis are provided. 2. The compound of claim 1 , wherein R is an unsubstituted C6-C50 alkyl or unsubstituted C6-C50 alkenyl.3. The compound of claim 1 , wherein R is an unsubstituted C10-C25 alkyl or unsubstituted C10-C25 alkenyl.4. The compound of claim 1 , wherein the sum of w claim 1 , x claim 1 , y claim 1 , and z is 20.6. The compound of claim 1 , wherein R is n-decyl claim 1 , n-undecyl claim 1 , n-dodecyl claim 1 , n-hexadecyl claim 1 , or n-heptadecyl.10. The method of claim 9 , wherein forming a trimethylsilyl derivative of compound of Formula (II) is done by contacting a compound of Formula (II) with a silylating agent in a suitable solvent.11. The method of claim 9 , wherein the silylating agent is hexamethyldisilazane (HMDS).12. The method of claim 9 , wherein the reducing agent is 1 claim 9 ,1 claim 9 ,3 claim 9 ,3-tetramethyldisiloxane.13. The method of claim 9 , wherein step (b) is performed at a temperature ranging from about 25° C. to about 80° C.14. The method of claim 9 , wherein step (b) does not require a solvent.15. The method of claim 9 , further comprising contacting the product of step (b) with water.16. A non-ionic polyether surfactant prepared by the method of .17. A surfactant composition comprising a compound of . This application claims the benefit of U.S. Application No. 63/053,426, filed Jul. 17, 2020, expressly incorporated herein by reference in its entirety.Polysorbates are amphiphilic, nonionic surfactants comprising fatty acid esters of polyoxyethylene sorbitan. Polysorbates are widely as research reagents and in protein pharmaceuticals to stabilize the proteins against interface-induced aggregation and to minimize surface adsorption of proteins. The main disadvantage of polysorbates is their susceptibility to hydrolysis due to the presence of an ester bond. Acid- and base-promoted hydrolytic degradation as well as enzymatic degradation of polysorbates is well- ...

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Номер записи: 38
08-01-2015 дата публикации

HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE

Номер: US20150011511A1
Автор: IKEHARA OSAMU, KODAMA Yuko, KONISHI Atsushi, Koshiba Takahiro, Ohsumi Koji, Suzuki Tamotsu, Tokumasu Munetaka
Принадлежит: AJINOMOTO CO., INC.

Compounds represented by formula (I): 122-. (canceled)25. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a halogeno group.27. A method according to claim 23 , wherein X is a lower alkylene group optionally having substituent(s) or a lower alkenylene group optionally having substituent(s) claim 23 , wherein said substituent(s) is selected from the group consisting of a halogeno group claim 23 , a hydroxyl group claim 23 , an amino group claim 23 , a lower alkyl group claim 23 , a lower alkoxyl group claim 23 , and a lower acyl group.28. A method according to claim 23 , wherein Y is a carbonyl group or a sulfonyl group.30. A method according to claim 29 , wherein R60 is a carboxyl group claim 29 , a sulfo group claim 29 , a lower alkoxycarbonyl group claim 29 , or a hydroxyl group claim 29 ,D is a lower alkylene group optionally having substituent(s), wherein said substituent(s) is selected from the group consisting of a halogeno group, a hydroxyl group, a thiol group, an amino group, a guanidino group, a carboxyl group, a sulfo group, a lower alkoxyl group, a lower alkylthio group, a lower alkylamino group, a lower acylamino group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkylsulfonylamino group, an arylsulfonylamino group optionally having substituent(s), an aryl group optionally having substituent(s), a heterocyclic group optionally having substituent(s), and an oxo group, andR70 is a hydrogen atom, a hydroxyl group, a lower alkyl group optionally having substituent(s), or a lower alkoxyl group optionally having substituent(s),or R70 and D may be bonded to form a cyclic amino group optionally having substituent(s).31. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a fluorine atom ...

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Номер записи: 39
08-01-2015 дата публикации

2-((2S,3S,4R,5R)-5-((S)-3-AMINO-2-HYDROXYPROP-1-YL)-4-METHOXY-3-(PHENYLSULFONYLMETHYL)TETRAHYDROFURAN-2-YL)ACETALDEHYDE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Номер: US20150011776A1
Автор: ALBERICO Dino, Gorin Boris, PAN Ming, Rudolph Alena, SOUZA Fabio E.S.
Принадлежит:

Disclosed is a compound of formula 1, as shown below, where R, R, R, R, R, Rand Rare as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin. 3. The compound according to claim 2 , wherein Ris —CH—CH═CH claim 2 , —CH—CH═CH—CH claim 2 , —CH—CH═C(CH)or —CH—C(═O)H.47-. (canceled)8. The compound according to claim 1 , wherein one of Rand Ris H and the other is —CHSO—Ar.910-. (canceled)11. The compound according to claim 1 , wherein Ris methyl.13. The process according to claim 12 , comprising converting the primary alcohol function in the compound of formula 2 into a leaving group to form an intermediate claim 12 , followed by amination of the intermediate to form the compound of formula 1.1420-. (canceled)21. The process according to claim 12 , wherein Ris —CH—CH═CH(compound of formula 1b).23. The process according to claim 12 , wherein Ris H and Ris —CHSOAr.24. The process according to claim 12 , wherein Ris methyl.26. The process according to claim 25 , wherein the alcohol is oxidized to a ketone prior to conversion to the compound of formula 1.2737-. (canceled)39. The process according to claim 38 , wherein the conversion to form the compound of formula 3 is carried out using nucleophilic addition of an allyl silane.4041-. (canceled)4344-. (canceled)46. A process for preparation of the compound of formula 3 claim 38 , comprising the process as defined in .48. A process for preparation of the compound of formula 4 claim 42 , comprising the process as defined in .49. A process for preparation of a halichondrin analog claim 12 , comprising the process as defined in .50. (canceled) This application claims the benefit of and priority to U.S. Provisional patent application No. 61/581,164, filed Dec. 29, 2011. The content of the above-noted patent application is hereby expressly incorporated by reference ...

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Номер записи: 40
08-01-2015 дата публикации

PROCESS FOR SYNTHESIS OF SYN AZIDO EPOXIDE AND ITS USE AS INTERMEDIATE FOR THE SYNTHESIS OF AMPRENAVIR & SAQUINAVIR

Номер: US20150011782A1
Автор: Gadakh Sunita Khanderao, Rekula Reddy Santhosh, Sudalai Arumugam
Принадлежит:

Disclosed herein is a novel route of synthesis of syn azide epoxide of formula 5, which is used as a common intermediate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt-catalyzed hydrolytic kinetic resolution of racemic anti-(2SR,3SR)-3-azido-4-phenyl-1,2-epoxybutane (azido-epoxide). 2. The process according to claim 1 , wherein the allylic alcohol is aryl substituted or unsubstituted butene alcohol.3. The process according to claim 1 , wherein the Lewis acid is selected from the group consisting of BF3 claim 1 , anhyd. A1C13 claim 1 , PF5 claim 1 , TiC14 claim 1 , Ti(OiPr)4 claim 1 , zinc bromide and cerium(III) Chloride.4. The process according to claim 1 , wherein the source of azide anion is selected from inorganic azide such as sodium azide claim 1 , chlorine claim 1 , bromine claim 1 , and iodine azides or organic azide such as tosyl azide claim 1 , trimethylsilyl azide in suitable organic solvent.5. The process according to claim 1 , wherein the hydrolytic kinetic resolution is carried out in presence of (S claim 1 ,S)-Co(Salen)acetate complex in molar concentration in the range of 0.2-0.8 mol % in suitable organic solvent.6. An enantioselective synthesis of HIV protease inhibitors from syn azido epoxide of formula (+)-5 comprising converting said syn azido epoxide to said HIV protease inhibitors claim 1 , wherein said syn azido epoxide is prepared by a process comprising:i) subjecting allylic alcohol to epoxidation with m-chloroperbenzoic acid (mCPBA) to obtain racemic epoxy alcohol;ii) ring opening of epoxide with azide anion in presence of Lewis acid to produce the anti-azido alcohol, followed by selective tosylation of primary alcohol to afford tosylate;iii) treating tosylate with base to obtain racemic azido epoxide;iv) subjecting racemic azido epoxide to hydrolytic kinetic resolution to obtain corresponding 1,2-diol and syn azido epoxide ...

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Номер записи: 41
08-01-2015 дата публикации

OXIDATION PROCESS TO PRODUCE A CRUDE AND/OR PURIFIED CARBOXYLIC ACID PRODUCT

Номер: US20150011783A1
Автор: Bowers Bradford, JANKA MESFIN, Jenkins Jason, Lange David, Moody Paula, MORROW Michael, PARKER KENNY, PARTIN LEE, Shaikh Ashfaq, SHANKS Thomas, Sumner Charles
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid. 1. A carboxylic acid composition consisting essentially of furan-2 ,5-dicarboxylic acid solids , said solids comprising:(a) furan-2,5-dicarboxylic acid in an amount greater than 90 weight percent;(b) b* value less than 15; and(c) FFCA in a range of from about 0.1 to about 4.0 weight percent(d) EFCA in an amount from 0.1 to 4 wt %2. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 92 weight percent.3. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.4. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.5. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 94 weight percent.6. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.7. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.8. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 96 weight percent.9. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.10. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.11. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in ...

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Номер записи: 42
09-01-2020 дата публикации

PROCESSES FOR THE PREPARATION OF 2,5-FURANDICARBOXYLIC ACID AND INTERMEDIATES AND DERIVATIVES THEREOF

Номер: US20200010441A1
Автор: BOUSSIE Thomas R., DIAMOND Gary M., DIAS ERIC L., Herrmann Stanley, Lavrenko Mayya, Longmire James M., Murphy Vincent J., Sokolovskii Valery, Torssell Staffan, Zhu Guang
Принадлежит:

The present disclosure provides processes for the production of 2-5-furandicarboxylic acid (FDCA) and intermediates thereof by the chemocatalytic conversion of a furanic oxidation substrate. The present disclosure further provides processes for preparing derivatives of FDCA and FDCA-based polymers. In addition, the present disclosure provides crystalline preparations of FDCA, as well as processes for making the same. 1. (canceled)2. A process for producing a first 2 ,5-furandicarboxylic acid (FDCA) pathway product from a first furanic oxidation substrate , the process comprising:(a) contacting an oxidation feedstock comprising a first furanic oxidation substrate and a first oxidation solvent with oxygen in the presence of a first heterogeneous oxidation catalyst under conditions sufficient to form a reaction mixture for oxidizing the first furanic oxidation substrate to a first FDCA pathway product, and producing the first FDCA pathway product;wherein the first oxidation solvent is a multi-component solvent comprising water and a water-miscible aprotic organic solvent;wherein no base is added to the reaction mixture during (first) contacting step (a);wherein the first heterogeneous oxidation catalyst comprises a first solid support and a first noble metal, and{'sup': 2', '2, 'wherein the solid support comprises a specific surface area in the range of from or any number in between 20 m/g to 100 m/g.'}3. The process of claim 2 , wherein the first noble metal is selected from the group consisting of platinum claim 2 , gold claim 2 , and combinations thereof.4. The process of claim 2 , wherein the water-miscible aprotic organic solvent is selected from the group consisting of tetrahydrofuran claim 2 , a glyme claim 2 , dioxane claim 2 , a dioxolane claim 2 , dimethylformamide claim 2 , dimethylsulfoxide claim 2 , sulfolane claim 2 , acetone claim 2 , N-methyl-2-pyrrolidone (“NMP”) claim 2 , methyl ethyl ketone (“MEK”) claim 2 , and gamma-valerolactone;and, if the water- ...

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Номер записи: 43
03-02-2022 дата публикации

METHODS AND COMPOSITIONS FOR BIORENEWABLE POLYESTERS DERIVED FROM CAMPHORIC ACID

Номер: US20220033574A1
Автор: MILLER STEPHEN A., NSENGIYUMVA Olivier
Принадлежит:

In one aspect, the disclosure relates to biorenewable polyesters and polyester copolymers derived from camphoric acid, methods of making same, and articles comprising same. The disclosed biorenewable polyesters can have a Mn of from about 5,000 Da to about 500,000 Da. Also disclosed herein is the preparation of various monomers useful in the reactions disclosed herein, e.g., cis-1,4-anhydroerythritol and bis(2-hydroxyethyl) camphorate. In various aspects, the disclosed biorenewable polyesters and polyester copolymers can be used to the production of various articles utilizing a conventional polyester or polyester copolymer, that is, to replace, in part or in whole, a conventional nonbiorenewable polyester or polyester copolymer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. 145-. (canceled)47. The polyester polymer of claim 46 , wherein Ris hydrogen.51. The polyester polymer of claim 46 , wherein number average molecular weight (M) is from about 7 claim 46 ,300 to about 20 claim 46 ,200 Da.52. The polyester polymer of claim 46 , wherein the dispersity is from about 2.7 to about 4.4.53. The polyester polymer of claim 46 , wherein the glass transition temperature (T) is from about −16° C. to about 125° C.54. The polyester polymer of claim 46 , wherein the temperature at which 5% mass loss under nitrogen is observed according to thermogravimetric analysis (T5) is from about 322° C. to about 368° C.55. The polyester polymer of claim 46 , wherein the polymer is non-crystalline.57. The polyester copolymer of claim 56 , wherein Ris hydrogen.62. The polyester copolymer of claim 56 , wherein the number average molecular weight (M) is from about 13 claim 56 ,300 to about 23 claim 56 ,800 Da.63. The polyester copolymer of claim 56 , wherein the dispersity is from about 2.3 to about 2.9.64. The polyester copolymer of claim 56 , wherein the glass transition temperature (T ...

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Номер записи: 44
19-01-2017 дата публикации

USE OF CARBOXYLIC ACIDS AND FURANIC MOLECULES FOR ESTERIFICATION

Номер: US20170015643A1
Автор: Stensrud Kenneth F., Venkitasubramanian Padmesh
Принадлежит:

A process for recovering and using an organic/carboxylic acid or furanic molecule by means of making an ester of a free carboxylic acid or furanic molecule with an alcohol in carbon dioxide (CO) without the presence of any other acid catalyst at a reaction temperature and pressure that corresponds to supercritical, critical or near critical conditions for the alcohol and/or COis described. The process can constitute part of a general process of refining carboxylic acids derived from a fermentation broth or use in the production of a variety of chemical compounds, such as Cplatform compounds or polymers. 1. A process for recovering and converting a carboxylic acid or a furanic molecule comprising: a) converting an aldose sugar to a sugar acid either by a chemical or biological means; b) bio-transforming said sugar acid to a keto-acid intermediate or furanic molecule in a solution; c) adjusting pH value of said solution containing said keto-acid intermediate or furanic molecule to a pH of less than 5 so as to generate free acids; and d) reacting said free acids with an alcohol and COto generate an ester of said carboxylic acid , keto-acid intermediate or furanic molecule.2. The process according to claim 1 , wherein said process further comprises drying said solution containing said keto-acid intermediate or furanic molecule.3. The process according to claim 1 , wherein said carboxylic acid is selected from the group consisting of: aldaric acids claim 1 , aldonic acids claim 1 , or uronic acids of a hexose or a pentose claim 1 , and a mixture thereof.4. The process according to claim 3 , wherein said aldaric acid is selected from the group consisting of: allaric acid claim 3 , altraric acid claim 3 , glucaric acid claim 3 , galactaric acid claim 3 , mannaric acid claim 3 , gularic acid claim 3 , idaric acid claim 3 , talaric acid claim 3 , xylaric acid claim 3 , lyxaric acid claim 3 , arabinaric acid claim 3 , and ribaric acid.5. The process according to claim 3 , ...

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Номер записи: 45
19-01-2017 дата публикации

PHOSPHONIC ACID CATALYST IN DEHYDRATIVE CYCLIZATION OF 5 AND 6 CARBON POLYOLS WITH IMPROVED COLOR AND PRODUCT ACCOUNTABILITY

Номер: US20170015676A1
Автор: Hagberg Erik, Stensrud Kenneth
Принадлежит:

A process for preparing materials derived from sugar alcohols such that the dehydration products exhibit better accountability and improved color to water-clear or near water-white appearance is described. In particular, the process involves employing a reducing Brønsted acid (e.g., phosphonic acid) for the catalysis of sugar alcohols to their corresponding dehydrated-cyclized products. 1. A method for preparing a cyclic dehydration product from 5 or 6 carbon polyols comprising: reacting a 5 or 6 carbon polyol with a reducing Brønsted acid catalyst in a reaction mixture , at a temperature and for a time sufficient to convert said 5 or 6 carbon polyol to corresponding cyclic dehydration products in a product mixture , wherein at least 70% of the 5 or 6 carbon polyol is converted to the corresponding cyclic dehydration products.2. The method according to claim 1 , further comprising purifying said dehydration products by at least a means selected from the group consisting of chromatography claim 1 , crystallization claim 1 , and distillation.3. The method according to claim 1 , wherein said reducing Brønsted acid catalyst is phosphonic acid.4. The method according to claim 1 , wherein said product mixture has an opacity and color appearance that ranges from translucent claim 1 , with a medium brown to light honey color claim 1 , to transparent claim 1 , clear or near water-white color after completion of said reaction time claim 1 , without being subject to a purifying or decolorizing operation.5. The method according to claim 3 , wherein said product mixture exhibits a color appearance after completion of said reaction time that is lighter and more translucent relative to a product mixture prepared using sulfuric acid catalyst at a catalyst load of ≧0.1 mol % claim 3 , instead of the phosphonic acid catalyst for the same time and temperature.6. The method according to claim 3 , wherein said product mixture exhibits reduced levels of color body formation or ...

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Номер записи: 46
21-01-2016 дата публикации

Substituted (R)-3-(4-methylcarbamoyl-3-fluorophenylamino)tetrahydrofuran-3-encarboxylic acid (variants) and ester thereof, method for preparation and use

Номер: US20160016925A1
Автор: Ivachtchenko Alexandre Vasilievich, Kravchenko Dmitry Vladimirovich, Mitkin Oleg Dmitrievich, Trifilenkov Andrey Sergeevich, Vorebey Anton Aleksandrovich
Принадлежит:

The present invention relates to novel chemical compounds of the general formula 1—intermediate products in synthesis of androgen receptor inhibitors which are of interest as anticancer medicaments. The subject of the invention is also a method for preparation of novel compounds of the general formula 1.1—androgen receptor inhibitors.

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Номер записи: 47
21-01-2016 дата публикации

Process for Making 2,5-Furandicarboxylic Acid

Номер: US20160016926A1
Автор: Sanborn Alexandra
Принадлежит:

A process is described for converting HMF to FDCA, comprising dissolving a quantity of HMF in water to form an aqueous solution including HMF, combining the aqueous solution including HMF with an oxygen source in the presence of a homogeneous metal salt catalyst, but in the substantial absence of any solvent for the HMF and the homogeneous metal salt catalyst other than water, and under conditions which are effective for oxidizing HMF in the presence of the catalyst to form FDCA, and then recovering an FDCA precipitate.

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Номер записи: 48
15-01-2015 дата публикации

Cyclohexenone Compositions and Process for Making Thereof

Номер: US20150018567A1
Автор: CHEN Chih-Ming, Cheng Hsiu-Yi, Liu Sheng-Yung, Wen Wu-Che
Принадлежит: GOLDEN BIOTECHNOLOGY CORPORATION

Provided herein are processes of preparing cyclohexenone compounds useful for cancer treatments and/or diseases. 120-. (canceled)221. The process of claim , wherein X is an oxygen , Y is an oxygen.231. The process of claim , wherein each of R , Rand Rindependently is H , methyl , ethyl , propyl , butyl , pentyl or hexyl.25. The process of claim 24 , wherein X is an oxygen claim 24 , Y is an oxygen.26. The process of claim 24 , wherein each of R claim 24 , Rand Rindependently is H claim 24 , methyl claim 24 , ethyl claim 24 , propyl claim 24 , butyl claim 24 , pentyl or hexyl.27. The process of claim 21 , wherein said base is a lithium salt.28. The process of claim 27 , wherein said lithium salt is n-butyllithium.29. The process of claim 24 , wherein said enolate compound is prepared under basic conditions.30. The process of claim 24 , wherein said enol compound is prepared under acidic conditions.31. The process of claim 24 , wherein Ris an acyclic or cyclic acetal claim 24 , acyclic or cylic ketal claim 24 , dithio acetal claim 24 , dithio ketal claim 24 , cyclic dithio acetal claim 24 , cyclic dithio ketal claim 24 , substituted hydrazone claim 24 , oxime claim 24 , oxime derivative claim 24 , or oxazolidine.33. The compound of claim 32 , wherein R is a hydrogen claim 32 , C(═O)CH claim 32 , C(═O)CH claim 32 , or C(═O)CH34. The compound of claim 32 , wherein each of R claim 32 , Rand Rindependently is hydrogen claim 32 , methyl claim 32 , ethyl claim 32 , propyl claim 32 , butyl claim 32 , pentyl claim 32 , hexyl claim 32 , heptyl claim 32 , or octyl optionally substituted with a aryl or heteroaryl.35. The compound of claim 34 , wherein each of R claim 34 , and Ris methyl substituted with phenyl.36. The compound of claim 32 , wherein Ris halogen claim 32 , NH claim 32 , NHCH claim 32 , N(CH) claim 32 , OCH claim 32 , OCH claim 32 , C(═O)CH claim 32 , C(═O)CH claim 32 , C(═O)OCH claim 32 , C(═O)OCH claim 32 , C(═O)NHCH claim 32 , C(═O)NHCH claim 32 , C(═O)NH claim ...

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Номер записи: 49
17-04-2014 дата публикации

Fuels And Fuel Additives Production From Glycerol Conversion Using A Monohydric Alcohol And Heterogeneous Catalysis

Номер: US20140101988A1
Автор: FENG Maoqi, TAN Chee-Kai
Принадлежит: SOUTHWEST RESEARCH INSTITUTE

The present disclosure relates to a method of converting glycerol into organic reaction products. The method may include mixing glycerol with a monohydric alcohol. The mixture of glycerol and monohydric alcohol is then reacted in the presence of a heterogeneous nano-structured catalyst, wherein the monohydric alcohol is present at subcritical/supercritical temperatures and pressures. This converts the glycerol into one or more reaction products, wherein the reaction products include an oxygenated organic reaction product. Ninety percent or greater of the glycerol is converted. 1. A method of converting glycerol , comprising:mixing glycerol containing hydroxyl groups with methanol;reacting said glycerol and methanol in the presence of a heterogeneous nano-structured catalyst, wherein said methanol is present at a temperature of 200° C. or greater and a pressure of 1,140 psia or greater;converting said glycerol into one or more reaction products, wherein one or more of said hydroxyl groups of said glycerol is converted into alkyl, alkyl ether, carbonyl, cyclic ether or alkene functionality; andwherein 90% or greater of said glycerol is converted to said reaction products containing said converted hydroxyl functionality.2. The method of claim 1 , wherein said methanol is present at a temperature in the range of 200° C. to 400° C. and a pressure in the range of 2 claim 1 ,000 psia to 3 claim 1 ,500 psia.3. The method of claim 1 , wherein said methanol is present as a supercritical fluid.4. The method of claim 1 , wherein said heterogeneous nano-structured catalyst comprises a zeolite mineral.5. The method of claim 4 , wherein said heterogenous nano-structured catalyst includes a zeolite and an oxide claim 4 , wherein said zeolite is selected from the group consisting of zeolite X and zeolite Y claim 4 , and said oxide is selected from one or more of the following: alumina claim 4 , silica and aluminosilicate.6. The method of claim 1 , wherein said heterogeneous nano- ...

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Номер записи: 50
17-04-2014 дата публикации

COMPOSITIONS AND METHODS FOR PRODUCING CHEMICALS AND DERIVATIVES THEREOF

Номер: US20140106414A1
Автор: Kambourakis Spiros, MARTIN Kevin V.
Принадлежит: Synthetic Genomics, Inc.

The present invention provides methods for producing a product of one or more enzymatic pathways. The pathways used in the methods of the invention involve one or more conversion steps such as, for example, an enzymatic conversion of guluronic acid into D-glucarate (Step 7); an enzymatic conversion of 5-ketogluconate (5-KGA) into L-Iduronic acid (Step 15); an enzymatic conversion of L-Iduronic acid into Idaric acid Step 7b); and an enzymatic conversion of 5-ketocluconate into 4,6-dihydroxy 2,5-diketo hexanoate (2,5-DDH) (Step 16). In some embodiments the methods of the invention produce 2,5-furandicarboxylic acid (FDCA) as a product. The methods include both enzymatic and chemical conversions as steps. Various pathways are also provided for converting glucose into 5-dehdyro-4-deoxy-glucarate (DDG), and for converting glucose into 2,5-furandicarboxylic acid (FDCA). The methods also involve the use of engineered enzymes that perform reactions with high specificity and efficiency. Additional products that can be produce include metabolic products such as, but not limited to, guluronic acid, L-iduronic acid, idaric acid, glucaric acid. Any of the products can be produced using glucose as a substrate or using any intermediate in any of the methods or pathways of the invention. 1. A method for producing a product of an enzymatic or chemical pathway from a starting substrate , the pathway comprising one or more conversion steps selected from the group consisting of:an enzymatic conversion of guluronic acid into D-glucarate (Step 7);an enzymatic conversion of 5-ketogluconate (5-KGA) into L-Iduronic acid (Step 15);an enzymatic conversion of L-Iduronic acid into Idaric acid Step 7b); andan enzymatic conversion of 5-ketocluconate into 4,6-dihydroxy 2,5-diketo hexanoate (2,5-DDH) (Step 16);an enzymatic conversion of 1,5-gluconolactone to gulurono-lactone (Step 19).2. The method of wherein the one or more conversion steps is the enzymatic conversion of guluronic acid into D- ...

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Номер записи: 51
28-01-2016 дата публикации

PROCESS FOR THE PREPARATION OF 2,5-FURAN-DICARBOXYLIC ACID

Номер: US20160024039A1
Автор: Baars Hendrikus Jacob, de Sousa Dias Ana Sofia Vagueiro, Gruter Gerardus Johannes Maria, Mazoyer Etienne, McKay Benjamin, Sikkenga David Lee, Vreeken Victor Peter Charles
Принадлежит:

2,5-Furandicarboxylic acid and methyl acetate are prepared in a continuous process by introducing a 5-methoxymethylfurfural-containing feedstock, an oxygen-containing gas, an oxidation catalyst and an acetic acid-containing solvent into a reactor; allowing 5-methoxymethylfurfural to react with oxygen and acetic acid in the presence of the oxidation catalyst to yield 2,5-furandicarboxylic acid as main product and methyl acetate; withdrawing 2,5-furandicarboxylic acid-containing product from the reactor and recovering 2,5-furandicarboxylic acid product; and withdrawing a vaporous stream containing methyl acetate from the reactor. 1. A continuous process for the preparation of 2 ,5-furan-dicarboxylic acid and methyl acetate , comprising:introducing a 5-methoxymethyl furfural-containing feedstock, an oxygen-containing gas, an oxidation catalyst and an acetic acid-containing solvent into a reactor;allowing 5-methoxymethyl furfural to react with oxygen and acetic acid in the presence of the oxidation catalyst to yield 2,5-furan-dicarboxylic acid as main product and methyl acetate;withdrawing 2,5-furan-dicarboxylic acid-containing product from the reactor and recovering 2,5-furan-dicarboxylic acid product; andwithdrawing a vaporous stream containing methyl acetate from the reactor.2. The process according to claim 1 , wherein the feedstock comprises from 2 to 50% wt of 5-methoxymethyl furfural claim 1 , based on the weight of the feedstock claim 1 , catalyst and solvent.3. The process according to claim 1 , wherein the feedstock claim 1 , in addition to 5-methoxymethyl furfural claim 1 , comprises up to 20% wt 5-hydroxymethyl furfural claim 1 , based on the weight of the feedstock.4. The process according to claim 1 , wherein the feedstock consists for 50 to 100% wt claim 1 , in particular from 90 to 100% wt of 5-methoxymethyl furfural.5. The process according to claim 1 , wherein the oxygen-containing gas being introduced into the reactor comprises from 6 to 22% vol ...

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Номер записи: 52
28-01-2016 дата публикации

FURANYL COMPOUNDS AND THE USE THEREOF

Номер: US20160024040A1
Автор: Chan Kyle W.H., Fung Leah M., Swindlehurst Cathy A.
Принадлежит:

Provided herein are substituted furanyl compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate eIF4E activity. In one embodiment, the compounds provided herein modulate the Hedgehog pathway activity. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders. 2. The compound of claim 1 , wherein L is S(O).3. The compound of claim 1 , wherein L is C(O).87. A pharmaceutical composition comprising a compound of any one of - claims 1 , or an enantiomer claims 1 , a mixture of enantiomers claims 1 , or a mixture of two or more diastereomers thereof claims 1 , or a pharmaceutically acceptable salt claims 1 , solvate claims 1 , hydrate claims 1 , or prodrug thereof claims 1 , and at least one pharmaceutically acceptable excipient or carrier.9. The pharmaceutical composition of claim 8 , further comprising one or more additional active agents.107. A method of treating claim 8 , preventing claim 8 , or ameliorating one or more symptoms of a disorder mediated by cap-dependent protein translation claim 8 , comprising administering a compound of any one of - claim 8 , or an enantiomer claim 8 , a mixture of enantiomers claim 8 , or a mixture of two or more diastereomers thereof claim 8 , or a pharmaceutically acceptable salt claim 8 , solvate claim 8 , hydrate claim 8 , or prodrug thereof claim 8 , or a pharmaceutical composition of or .117. A method of treating claim 8 , preventing claim 8 , or ameliorating one or more symptoms of a disorder mediated by eIF4E claim 8 , comprising administering a compound ...

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Номер записи: 53
26-01-2017 дата публикации

SYNTHETIC PROCESS FOR PREPARING 2-((2-ETHOXY-2-OXOETHYL)(METHYL)AMINO)-2-OXOETHYL 5-TETRADECYLOXY)FURAN-2-CARBOXYLATE

Номер: US20170022176A1
Автор: Khumtaveeporn Kanjai, Krasik Pavel, SHAW Anthony Adrian
Принадлежит:

Disclosed herein are processes for forming 2-((2-ethoxy-2-oxoethyl)(methyl)amino)-2-oxoethyl 5-tetradecyloxy)furan-2-carboxylate: 2. The process of wherein X is halogen.3. The process of wherein X is Cl.4. The process of wherein the ether solvent has a boiling point of below 100° C.5. The process of wherein the ether solvent is dialkyl ether.6. The process of wherein the dialkyl ether is methyl t-butyl ether.7. The process of wherein Ris —CHand Ris ethyl.9. The process of wherein the coupling is carried out at temperature below 10° C.10. The process of wherein the ether solvent is methyl t-butyl ether.11. The process of wherein the base is an organic base.12. The process of wherein the organic base is triethylamine or trimethylamine.14. The process of wherein X is Cl.15. The process of wherein the solvent is dialkyl ether.16. The process of wherein the dialkyl ether is methyl t-butyl ether.17. The process of wherein the organic base is triethylamine or trimethylamine.18. The process of wherein Ris —CHand Ris ethyl.20. The process of wherein the coupling is carried out at temperature below 10° C. in the presence of potassium bicarbonate. This application is a Continuation of U.S. patent application Ser. No. 15/015,828, filed Feb. 4, 2016; which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 62/112,569, filed Feb. 5, 2015, which application is incorporated herein by reference in its entirety.Technical FieldThis disclosure is generally related to a synthetic process for preparing 2-((2-ethoxy-2-oxoethyl)(methyl)amino)-2-oxoethyl 5-tetradecyloxy)furan-2-carboxylate, a prodrug of a fatty acid mimetic.BackgroundFatty acid synthesis starts with the carboxylation of acetyl CoA to malonyl CoA. This irreversible reaction is the committed step in fatty acid synthesis. The synthesis of malonyl CoA is catalyzed by acetyl CoA carboxylase (ACC) (See, Brownsey, R. W. et al., “Regulation of acetyl-CoA carboxylase”, . (2006) 34: 223-227). ...

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Номер записи: 54
26-01-2017 дата публикации

Neuraminidase Inhibitor Compounds, Compositions and Methods for the Use Thereof in Anti-Viral Treatments

Номер: US20170022177A1
Автор: Kim Jin Hyo, Watts Andrew Graham, Wennekes Tom, Withers Stephen
Принадлежит:

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza. 3. The compound of claim 1 , wherein T is COOH or COOR claim 1 ,{'sup': '1', 'sub': '1-20', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}4. The compound of claim 1 , wherein T is C(O)OCH claim 1 , C(O)OCHCH claim 1 , C(O)OCHCHCH claim 1 , C(O)OCHCHCHCH claim 1 , C(O)OCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCHCH claim 1 , or COOH.5. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO.6. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , and OR claim 1 ,{'sup': '3', 'sub': '1-20', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}7. The compound of claim 1 , wherein A is F or Cl.8. The compound of claim 1 , wherein A is F.9. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO claim 1 , provided A and D are not both H.10. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , and Cl claim 1 , provided A and D are not both H.11. The compound of claim 1 , wherein D is F or Cl.12. ...

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Номер записи: 55
24-01-2019 дата публикации

METHOD FOR PRODUCING PURIFIED DIALKYL-FURAN-2,5-DICARBOXYLATE

Номер: US20190023676A1
Автор: Janka Mesfin Ejerssa
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is a purified dialkyl furan dicarboxylate (DAFD) vapor composition containing at least 99.5 wt. % DAFD; 5-(alkoxycarbonyl) furan-2-carboxylic acid (ACFC) that, if present, is present in an amount of not more than 1000 ppm, alkyl-5-formylfuran-2-carboxylate (AFFC) that, if present, is present in an amount of not more than 1000 ppm, 5-(dialkoxymethyl)furan-2-carboxylic acid (DAFCA) that if present, is present in an amount of not more than 1000 ppm, and alkyl 5-(dialkoxymethyl)furan-2-carboxylate (ADAFC) that if present, is present in an amount of not more than 1000 ppm, in each case based on the weight of the DAFD vapor composition. 3. A purified liquid DAFD composition comprising:(i) at least 99.5 wt. % liquid DAFD;(ii) 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC) that if present, is present in an amount of not more than 1000 ppm,(iii) alkyl-5-formylfuran-2-carboxylate (AFFC) that if present, is present in an amount of not more than 1000 ppm,(iv) 5-(dialkoxymethyl)furan-2-carboxylic acid (DAFCA) that if present, is present in an amount of not more than 1000 ppm,(v) alkyl 5-(dialkoxymethyl)furan-2-carboxylate (ADAFC) that if present, is present in an amount of not more than 1000 ppm,(vi) not more than 1 wt. % water, and(vii) not more than 1 wt. % solids,in each case based on the weight of the purified liquid DAFD composition.4. The purified liquid DAFD composition of claim 3 , wherein the liquid is not subjected to further purification.5. The purified liquid DAFD composition of claim 3 , wherein the liquid is loaded into a pipeline claim 3 , a tanker car claim 3 , or rail car.6. A solids DAFD composition comprising solid particles of DAFD claim 3 , wherein said solids comprise:(i) at least 99.5 wt. % DAFD;(ii) 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC) that if present, is present in an amount of not more than 1000 ppm,(iii) alkyl-5-formylfuran-2-carboxylate (AFFC) that if present, is present in an amount of not more than 1000 ppm,(iv) 5-( ...

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Номер записи: 56
28-01-2021 дата публикации

PROCESSES FOR PREPARING 2,5-FURANDICARBOXYLIC ACID AND ESTERS THEREOF

Номер: US20210024480A1
Автор: Metkar Pranit S, Ozer Ronnie, RAJAGOPALAN BHUMA
Принадлежит:

A process for producing furan dicarboxylic acid or an ester thereof from a feedstock comprising hydroxymethyl furfural (HMF) and humins is disclosed. Humins are a byproduct from reactions forming HMF from sugars and are typically removed from the HMF prior to any further processing. A humins-containing HMF feedstock is utilized to produce furan dicarboxylic acids and ester substantially free from humins. 1. A process comprising:a) oxidizing a feedstock comprising hydroxymethyl furfural and humins to produce a mixture comprising crude humins-containing 2,5-furan dicarboxylic acid;b) separating the mixture to obtain a solid 2,5-furan dicarboxylic acid/humins composition;c) esterifying the solid 2,5-furan dicarboxylic acid/humins composition with an alcohol to produce a crude ester of 2,5-furan dicarboxylic acid; andd) purifying the crude ester of 2,5-furan dicarboxylic acid obtained in step c) by distillation or by sublimation to produce a purified ester of 2,5-furan dicarboxylic acid substantially free of humins.2. The process of wherein the purified ester of 2 claim 1 ,5-furan dicarboxylic acid is 2 claim 1 ,5-furan dicarboxylic acid dimethyl ester.3. A process comprising:i) oxidizing a feedstock comprising hydroxymethyl furfural and humins in a solvent to produce a mixture comprising crude humins-containing 2,5-furan dicarboxylic acid;ii) filtering the mixture under high temperature to obtain a filtrate comprising 2,5-furan dicarboxylic acid substantially free of humins, wherein the filtration temperature is sufficiently high to keep the 2,5-furan dicarboxylic acid soluble in the solvent;iii) esterifying the 2,5-furan dicarboxylic acid substantially free of humins with an alcohol to produce a crude ester of 2,5-furan dicarboxylic acid; andiv) purifying the crude ester of 2,5-furan dicarboxylic acid obtained in step iii) by distillation or sublimation to obtain a purified ester.4. The process of wherein the ester of 2 claim 3 ,5-furan dicarboxylic acid is 2 claim 3 ...

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Номер записи: 57
01-02-2018 дата публикации

DERMATOLOGICAL FORMULATIONS OF 2-(2-ETHOXY-2-OXOETHYL)(METHYL)AMINO-2-OXOETHYL 5-(TETRADECYLOXY)FURAN-2-CARBOXYLATE

Номер: US20180028487A1
Автор: Khumtaveeporn Kanjai, Krasik Pavel, SHAW Anthony Adrian
Принадлежит:

Disclosed herein are dermatological formulations comprising low-impurity TOFA prodrug 2-(2-ethoxy-2-oxoethyl)(methyl)amino-2-oxoethyl 5-(tetradecyloxy)furan-2-carboxylate represented by Formula (Ia) and pharmaceutical use thereof: 3. The drug product composition of wherein Ris —CH claim 1 , —CH claim 1 , —CH claim 1 , —CH claim 1 , or —CH.4. The drug product composition of wherein Ris hydrogen or methyl.5. The drug product composition of wherein X is bromo or chloro.6. The drug product composition of wherein the one or more impurities represented by Formula (IV) are no more than 2% w/w of the drug product composition.7. The drug product composition of wherein the one or more impurities represented by Formula (II) are no more than 120 ppm of the drug product composition.8. The drug product composition of wherein the byproduct represented by Formula (VI) claim 1 , wherein Ris hydrogen claim 1 , is no more than 0.5% w/w of the drug product composition.9. The drug product composition of wherein the one or more impurities represented by Formula (V) are no more than 0.2% w/w of the drug product composition.11. The dermatological formulation of wherein the one or more impurities together are no more than 2% w/w of the compound of Formula (I).13. The dermatological formulation of wherein Ris —CH claim 10 , —CH claim 10 , —CH claim 10 , —CH claim 10 , or —CH.14. The dermatological formulation of wherein Ris hydrogen or methyl.15. The dermatological formulation of wherein X is bromo or chloro.16. The dermatological formulation of wherein the one or more impurities represented by Formula (IV) are no more than 2% w/w of the compound of Formula (I).17. The dermatological formulation of wherein the one or more impurities represented by Formula (II) are no more than 120 ppm of the compound of Formula (I).18. The dermatological formulation of wherein the impurity represented by Formula (VI) claim 10 , wherein Ris hydrogen claim 10 , is no more than 0.5% w/w of the compound of ...

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Номер записи: 58
04-02-2016 дата публикации

METHOD OF MANUFACTURING DICARBOXYLIC ACIDS AND DERIVATIVES FROM COMPOSITIONS COMPRISING KETOCARBOXYLIC ACIDS

Номер: US20160031788A1
Автор: Molitor Erich J., MULLEN Brian D.
Принадлежит:

A crude composition comprising a ketocarboxylic acid such as levulinic acid, derived from biomass in an aqueous phase comprising impurities, can be efficiently converted in high yield to the corresponding dicarboxylic acid, such as succinic acid, which can be purified and dried. 2. The method of claim 1 , wherein the oxidizing agent is nitric acid and optionally a catalyst comprising vanadium pentoxide claim 1 , and optionally in the further presence of a metallic nitrite.3. The method of claim 1 , wherein the crude composition is an acidic hydrolysate of the biomass and comprises at least 5 wt. % water.4. The method of claim 1 , wherein the hydrolysate is obtained employing concentrated sulfuric acid.5. (canceled)6. The method of claim 1 , further comprising removing char particles from the crude composition prior to oxidizing the ketocarboxylic acid to the corresponding dicarboxylic acid.7. The method of claim 1 , wherein the oxidizing agent comprises nitric acid and further 0.1 to 1.0% by weight claim 1 , calculated on the basis of nitric acid claim 1 , of sodium nitrite is added.8. The method of claim 1 , wherein Ris C-Calkyl and a=1-3.9. (canceled)10. (canceled)11. The method of claim 1 , wherein the ketocarboxylic acid is obtained from a biomass conversion in the presence of an acid catalyst comprising a Brønsted-Lowry acid claim 1 , a Lewis acid claim 1 , or a combination that comprises at least one of the foregoing catalysts.12. The method of claim 1 , wherein the crude composition comprising the ketocarboxylic acid comprises at least 5 wt. % of impurities comprising biomass residue claim 1 , solid humins claim 1 , extraction solvent claim 1 , reaction by-products claim 1 , reactants claim 1 , and combinations thereof.13. (canceled)14. The method of claim 1 , wherein the impurities comprise furfural claim 1 , formic acid claim 1 , furfuryl alcohol claim 1 , hydroxymethyl furfural claim 1 , angelica lactone claim 1 , acetic acid claim 1 , methanol claim 1 , ...

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Номер записи: 59
29-01-2015 дата публикации

ESTERIFICATION OF FURAN-2,5-DICARBOXYLIC ACID TO A DIALKYL-FURAN-2,5-DICARBOXYLATE VAPOR WITH RECTIFICATION

Номер: US20150031903A1
Автор: Janka Mesfin Ejerssa, Parker Kenny Randolph, Partin Lee Reynolds, Shaikh Ashfaq
Принадлежит:

A process for the manufacture of dialkyl furan-2,5-dicarboxylate (DAFD) vapor composition by feeding furan-2,5-dicarboxylic acid (“FDCA”) to an esterification reactor and in the presence of an alcohol compound such as methanol, conducting an esterification reaction to form an esterification vapor containing DAFD, unreacted alcohol compound, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and water, and continuously passing the esterification vapor through an ACFC condensing zone, that can be integral with the esterification reactor, in which at least a portion of the ACFC in the esterification vapor is converted to a liquid phase condensate, and continuously discharging the esterification vapor from the ACFC condensing zone as a DAFD vapor. There is also a DAFD vapor composition containing DAFD, water, unreacted alcohol, and by-products. 1. A vapor stream discharged from a rectification zone of a dialkyl furan-2 ,5-dicarboxylate (DAFD) manufacturing process , said vapor stream comprising:a. at least 2 wt. % alcohol;b. at least 1 wt. % DAFD;c. at least 0.5 wt. % water; and 'wherein said vapor stream has an ACFC:DAFD molar ratio not greater than 0.5:1.', 'd. from zero up to 3 wt. % 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC),'}2. The vapor stream of claim 1 , further comprising at least 0.5 wt. % alkyl furan-2-carboxylate (AFC).3. The vapor stream of claim 1 , further comprising at least 0.01 wt. % alkyl 5-formylfuran-2-carboxylate (AFFC).4. The vapor stream of claim 1 , wherein said alcohol is present in said vapor stream in an amount from at least 5 wt. % up to 50 wt. % claim 1 , wherein said DAFD is present in said vapor stream in an amount from at 2 wt. % least up to 50 wt. % claim 1 , wherein said water is present in said vapor stream in an amount from at least 2 wt. % up to 15 wt. % claim 1 , wherein said ACFC is present in said vapor stream in an amount from zero up to 2 wt. % claim 1 , wherein said vapor stream has an ACFC:DAFD molar ratio not greater ...

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Номер записи: 60
17-02-2022 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20220048876A1
Автор: Cassayre Jerome Yves, El Qacemi Myriem, Pitterna Thomas, Stoller Andre
Принадлежит: SYNGENTA PARTICIPATIONS AG

Compounds of formula (I), wherein the substituents are as defined in claim , and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, and their uses as insecticides. 2. The compound according to claim 1 , wherein Ais C—R; Ais C—H; Ais C—H; and Ais C—H claim 1 , wherein Ris halogen claim 1 , cyano claim 1 , nitro claim 1 , C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , C-Chaloalkyl or C-Calkenyl.3. The compound of formula (I) according to claim 1 , wherein Ris halogen claim 1 , C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , C-Chaloalkyl claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy or di-C-Calkylamino claim 1 , C-Calkylthio or C-Calkyloxycarbonyl.4. The compound of formula (I) according to claim 1 , wherein Ris hydrogen claim 1 , formyl claim 1 , C-Calkyl claim 1 , C-Calkylcarbonyl- or C-Calkoxycarbonyl-.5. The compound of formula (I) according to claim 1 , wherein Ris C-Calkyl claim 1 , C-Calkylcarbonyl- claim 1 , C-Ccycloalkylcarbonyl claim 1 , C-Calkoxy claim 1 , C-Calkoxy-C-Calkyl claim 1 , C-Calkoxycarbonyl claim 1 , C-CalkylcarbonyloxyC-Calkyl claim 1 , C-Calkoxycarbonylsulfanyl claim 1 , C-CalkylaminocarbonyloxyC-Calkyl claim 1 , C-CdialkylaminocarbonyloxyC-Calkyl claim 1 , C-CalkylaminocarbonylC-Calkyl claim 1 , C-CdialkylaminocarbonylC-Calkyl claim 1 , or C-CalkoxycarbonylC-CalkylaminoC-Calkyl claim 1 , wherein each alkyl or alkoxy group may be optionally substituted with from one to three halogen atoms6. The compound of formula (I) according to claim 4 , wherein Ris C-Ccyanoalkyl claim 4 , C-Calkoxy-C-Calkyl claim 4 , C-Calkoxycarbonyl or C-CalkylcarbonyloxyC-Calkyl.7. The compound of formula (I) according to claim 6 , wherein Ris cyanomethyl claim 6 , methoxymethyl claim 6 , ethoxymethyl claim 6 , methoxycarbonyl claim 6 , ethoxycarbonyl claim 6 , methylcarbonyloxymethyl claim 6 , 1-methylethylcarbonyloxymethyl or 1 claim 6 ,1-dimethylethylcarbonyloxymethyl.8. The compound according to claim 1 , wherein ...

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Номер записи: 61
17-02-2022 дата публикации

ALICYCLIC MUSK FRAGRANCE COMPOUNDS

Номер: US20220049183A1
Автор: CHANDRASEKARAN Vijayanand, Hölscher Bernd, OHRMANN Eva, WAGNER Tobias
Принадлежит:

The present invention primarily relates to the use of a compound according to the general formula (I) wherein i) m is 1, n is 1, o is 0 or 1, Y is Hydrogen, or ii) m is 2, n is 0, o is 1, Y is methyl, and wherein X is O or methylene, R and R1 are each methyl or form together with the carbon atom attached to a carbonyl group, and R2 is methyl, ethyl, propyl, butyl, butan-2-one-4-yl, tetrahydrofuran-2-yl, or tetrahydrofuran-3-yl, as perfuming ingredients. Moreover, the present invention relates to perfume compositions and perfumed products comprising the before mentioned perfuming ingredients. Still more particularly, the invention relates to a method for producing said perfumed products and a method of imparting and/or increasing musk odor characteristics to perfumed products. This invention also relates to a process for the preparation of said compounds according to the general formula (I). 14-. (canceled)6. A compound according to selected from the group consisting of 1-(3 claim 5 ,3-dimethylcyclohexyl)ethyl 4-oxopentanoate claim 5 , 2-(1-(3 claim 5 ,3-dimethylcyclohexyl)ethoxy)-2-methylpropyl tetrahydrofuran-2-carboxylate claim 5 , 1-(3 claim 5 ,3-dimethylcyclohexyl)ethyl 4-oxoheptanoate claim 5 , 1-(3 claim 5 ,3-dimethylcyclohexyl)ethyl 4-oxooctanoate claim 5 , 1-(3 claim 5 ,3-dimethylcyclohexyl)ethyl 3-oxohexanoate claim 5 , 1-(3 claim 5 ,3-dimethylcyclohexyl)ethyl 3-oxoheptanoate claim 5 , 2-(1-(3 claim 5 ,3-dimethylcyclohexyl)ethoxy)-2-oxoethyl 4-oxopentanoate claim 5 , 2 claim 5 ,6 claim 5 ,6-trimethylcycloheptyl 4-oxopentanoate claim 5 , and 2-oxo-2-((2 claim 5 ,6 claim 5 ,6-trimethylcycloheptyl)oxy)ethyl 4-oxopentanoate.7. A perfume composition comprising a compound according to .8. A perfume composition according to comprising one or more additional fragrance ingredients.9. A perfumed product comprising a compound as according to .10. A perfumed product according to claim 9 , wherein the product is selected from the group consisting of perfume extraits ...

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Номер записи: 62
31-01-2019 дата публикации

LOW PRESSURE, HIGH TEMPERATURE PROCESS FOR FORMING 2,5-FURANDICARBOXYLIC ACID DIALKYL ESTER

Номер: US20190031633A1
Автор: CIPOT-WECHSLER JUDY H., Metkar Pranit S., Ozer Ronnie
Принадлежит:

Processes for preparing a dialkyl ester of 2,5-furan dicarboxylic acid are disclosed. The processes comprise contacting 2,5-furan dicarboxylic acid with excess alcohol and, optionally, a catalyst at a pressure in the range of between 1 bar and 21 bar and a temperature in the range of from 65° C. to 325° C. to form a vapor reaction product comprising an ester of 2,5-furan dicarboxylic acid, the alcohol and water; and distilling the vapor reaction product at a pressure in the range of from 0 bar to 3.5 bar at a temperature in the range of from 38° C. to 204° C. to separate the water and alcohol from the ester of 2,5-furan dicarboxylic acid. 1. A process comprising:a) contacting 2,5-furan dicarboxylic acid with excess alcohol and, optionally, a catalyst at a pressure in the range of between 1 bar and 21 bar and a temperature in the range of from 65° C. to 325° C. to form a vapor reaction product comprising an ester of 2,5-furan dicarboxylic acid, the alcohol and water; andb) distilling the vapor reaction product at a pressure in the range of from 0 bar to 3.5 bar at a temperature in the range of from 38° C. to 204° C. to separate the water and alcohol from the ester of 2,5-furan dicarboxylic acid.2. The process of claim 1 , wherein the pressure of step a) is in the range of from 1 bar to 6 bar.3. The process of claim 1 , wherein the catalyst claim 1 , if present claim 1 , is cobalt (II) acetate claim 1 , iron (II) chloride claim 1 , iron (III) chloride claim 1 , iron (II) sulfate claim 1 , iron (III) sulfate claim 1 , iron (II) nitrate claim 1 , iron (III) nitrate claim 1 , iron (II) oxide claim 1 , iron (III) oxide claim 1 , iron (II) sulfide claim 1 , iron (III) sulfide claim 1 , iron (II) acetate claim 1 , iron (III) acetate claim 1 , magnesium (II) acetate claim 1 , magnesium (II) hydroxide claim 1 , manganese (II) acetate claim 1 , phosphoric acid claim 1 , sulfuric acid claim 1 , zinc (II) acetate claim 1 , zinc stearate claim 1 , a solid acid catalyst claim 1 , ...

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Номер записи: 63
31-01-2019 дата публикации

REACTIVE DISTILLATION PROCESS FOR THE ESTERIFICATION OF FURANDICARBOXYLIC ACID

Номер: US20190031634A1
Автор: Metkar Pranit S., Sengupta Sourav Kumar
Принадлежит:

Disclosed are processes for producing the dialkyl ester of 2,5-furan dicarboxylic acid by contacting a feed containing 2,5-furan dicarboxylic acid and a high boiling solvent with an alcohol in the presence of a solid acid catalyst using reactive distillation. 1. A process comprising:a) providing a reactive distillation column comprising a top, a bottom, and a reaction zone in between the top and the bottom, and a solid acid catalyst situated in the reaction zone;b) contacting a feed comprising 2,5-furan dicarboxylic acid and a high boiling solvent with an alcohol in the reaction zone at a temperature in the range of 40° C. to 300° C. and a pressure in the range of 0.0007 MPa to 3.4 MPa for a residence time sufficient to produce a mixture comprising a dialkyl ester of 2,5-furan dicarboxylic acid and water;c) removing a vapor mixture comprising the alcohol and water from the top of the reactive distillation column;d) collecting a product stream comprising the dialkyl ester of 2,5-furan dicarboxylic acid, the high boiling solvent, and optionally one or more of a monoalkyl ester of 2,5-furan dicarboxylic acid, any unreacted 2,5-furan dicarboxylic acid and any other high boilers from the bottom of the reactive distillation column; ande) separating the dialkyl ester of 2,5-furan dicarboxylic acid from the product stream using distillation.2. The process of wherein the high boiling solvent comprises at least one of dimethyl sulfoxide claim 1 , dimethylacetamide claim 1 , sulfolane claim 1 , dimethyl ester of 2 claim 1 ,5-furan dicarboxylic acid claim 1 , gamma-valerolactone claim 1 , gamma-butyrolactone claim 1 , isosorbide dimethyl ether claim 1 , propylene carbonate claim 1 , adipic acid claim 1 , isosorbide claim 1 , isophorone claim 1 , ethyl phenyl ether claim 1 , diphenyl ether claim 1 , dibenzyl ether claim 1 , aromatic 200 fluid claim 1 , butyl phenyl ether claim 1 , methyl heptyl ketone claim 1 , ethyl phenyl ketone claim 1 , 2′-hydroxyacetophenone claim 1 , ...

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Номер записи: 64
04-02-2021 дата публикации

CONVERSION OF 1,2,5,6-HEXANETETROL (HTO) TO TETRAHYDROFURAN dicarboxylic acid (THFDCA)

Номер: US20210032215A1
Автор: Ma Chi-Cheng
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

Disclosed herein are methods for synthesizing useful intermediates and/or products from 1,2,5,6-hexanetetrol (HTO), which itself can be derived from a sugar. In an aspect, a process is provided for production of THFDCA from 1,2,5,6-hexanetetrol (HTO). The process comprises the steps of (a) ring closing to form a ring compound and (b) oxidizing using a catalyst comprising platinum and bismuth to form an acid mixture. Step (a) may be performed before or after step (b). 1. A process for synthesizing tetrahydrofuran-2 ,5-dicarboxylic acid (THFDCA) , the process comprising:(a) ring closing to form a ring compound; and(b) oxidizing using a catalyst comprising platinum and bismuth to form an acid mixture;wherein step (a) may be performed before or after step (b);wherein when step (a) is performed before step (b), then step (a) comprises contacting 1,2,5,6-hexanetetrol (HTO) with an acid for a time sufficient to form the ring compound, wherein the formed ring compound is tetrahydrofuran dimethanol; and step (b) comprises oxidizing the tetrahydrofuran dimethanol formed in step (a) while the tetrahydrofuran dimethanol is in contact with the catalyst such that an acid mixture is formed comprising at least one of THFDCA or 2,5-anhydro-3,4-dideoxy-hexanoic acid, and when 2,5-anhydro-3,4-dideoxy-hexanoic acid is formed as part of the acid mixture, i) recovering the 2,5-anhydro-3,4-dideoxy-hexanoic acid from the acid mixture, ii) recovering the 2,5-anhydro-3,4-dideoxy-hexanoic acid from the acid mixture and oxidizing the same while in contact with a catalyst comprising platinum and bismuth to form THFDCA, or iii) oxidizing the 2,5-anhydro-3,4-dideoxy-hexanoic acid in the acid mixture while in contact with the catalyst used in step b) to form additional THFDCA;wherein when step (b) is performed before step (a), then step (b) comprises oxidizing 1,2,5,6-hexanetetrol (HTO) while the HTO is in contact with the catalyst such that an acid mixture comprising 2,5-dihydroxyadipic acid and ...

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Номер записи: 65
08-02-2018 дата публикации

INTERMEDIATES AND METHODS FOR THE SYNTHESIS OF HALICHONDRIN B ANALOGS

Номер: US20180037588A1
Автор: Chase Charles E., Endo Atsushi, Fang Francis G., LI Jing
Принадлежит:

Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described. 6. The method of claim 2 , further comprising producing the compound of formula (I) by crystallizing said compound from a mixture of diastereomers under appropriate crystallization conditions.7. The method of claim 1 , further comprising producing the compound of formula (II) by crystallizing said compound from a mixture of diastereomers under appropriate crystallization conditions.10. The method of claim 8 , wherein at least one of Land Lis a protecting group selected from the group consisting of methoxymethyl claim 8 , trimethylsilyl claim 8 , triethylsilyl claim 8 , t-butyldimethylsilyl claim 8 , t-butyldiphenylsilyl claim 8 , triisopropylsilyl claim 8 , methyl claim 8 , t-butyl claim 8 , 3 claim 8 ,4-dimethoxybenzyl claim 8 , p-methoxybenzyl claim 8 , benzyl claim 8 , and trityl claim 8 , or Land Ltogether are cycloheptylidine.11. The method of claim 8 , wherein at least one of Land Lis Calkyl carbonyl claim 8 , or Land Ltogether are acetonide claim 8 , benzylidene claim 8 , pyran claim 8 , cyclohexylidene claim 8 , or cyclopentylidene.15. The method of claim 13 , wherein the divalent protecting group is a cyclohexylidine protecting group.18. The compound of claim 17 , wherein at least one of Land Lis a protecting group selected from the group consisting of methoxymethyl claim 17 , trimethylsilyl claim 17 , triethylsilyl claim 17 , t-butyldimethylsilyl claim 17 , t-butyldiphenylsilyl claim 17 , triisopropylsilyl claim 17 , methyl claim 17 , t-butyl claim 17 , 3 claim 17 ,4-dimethoxybenzyl claim 17 , p-methoxybenzyl claim 17 , benzyl claim 17 , and trityl claim 17 , or Land Ltogether are cycloheptylidine.19. The compound of claim 17 , wherein at least one of Land Lis Calkyl carbonyl claim 17 , or Land Ltogether are acetonide claim 17 , benzylidene claim 17 , cyclohexylidene claim 17 , or cyclopentylidene. This application is a continuation of U.S. application ...

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Номер записи: 66
06-02-2020 дата публикации

NOVEL CITRIC ACID DERIVATIVE

Номер: US20200039964A1
Автор: ADACHI Masakazu, ADACHI Taro, HIRAISHI Katsuya, JIMMA Fumie, KAGAWA Tomohiro, SOMA Hiroyuki, YAMAOKA Ippei
Принадлежит:

Compounds (citric acid derivatives) represented by formulas (1) and (2) below are novel compounds having an inhibitory effect against liver disorder and can be used as liver disorder inhibitors and food additives (wherein Rrepresents a C1 to C3 alkyl group optionally having a carboxyl group or a hydroxyl group, and Rrepresents a hydrogen atom, or Rand Roptionally form a cyclic structure together to represent a C2 to C3 alkylene chain). 4. The method for inhibiting liver disorder according to claim 3 , wherein the liver disorder is nonalcoholic steatohepatitis (NASH).6. The method according to claim 3 , wherein the compound represented by formula (1) is allowed to react in an aqueous solution having a pH of 6.0 to 12.0 to which the alkaline substance for generating hydroxide ions is added claim 3 , at 80 to 130° C. for 20 minutes to 240 minutes. This application is a divisional of U.S. application Ser. No. 15/770,300 filed Apr. 23, 2018, which is a U.S. National Phase of PCT/JP2016/004789, filed on Nov. 1, 2016, which claims priority to Japanese Application No. 2015-216000, filed Nov. 2, 2015. The disclosure of each of these applications is herein incorporated by reference in its entirety.The present invention relates to a novel citric acid derivative, and more specifically, to a citric acid derivative having an inhibitory effect against liver disorder.Ume (Japanese apricot) () belongs to the subgenus of the genus of the subfamily Amygdaloideae of the family Rosaceae and is eaten in the form of processed products of ume such as pickled ume, ume wine, and ume extract (ume flesh extract). Further, ume extract has advantageous effects such as sterilization, treatment from fatigue, and stomach protection action, and thus ume extract has been taken for health. Further, ume extract is known to have an effect of improving bloodstream (see Non-patent Documents 1 and 2). It is known that the effect of improving bloodstream is derived from Mumefural which is produced by ...

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Номер записи: 67
15-02-2018 дата публикации

METHOD FOR MANUFACTURING FURAN-2,5-DICARBOXYLIC ACID (FDCA) FROM A SALT SOLUTION

Номер: US20180044312A1
Автор: DE HAAN André Banier, Van krieken Jan
Принадлежит: Purac Biochem BV

A method for manufacturing furan--dicarboxylic acid (FDCA) by converting a furan--dicarboxylate salt (MFDC) into FDCA, including the steps of combining an aqueous solution of MFDC with a concentration of at least 5 wt.% with an inorganic acid (HY), to form a reaction mixture including solid FDCA in a concentration of 1-15 wt.% in a salt solution resulting from the cation of furan--dicarboxylate salt and the anion of the inorganic acid (MY solution), removing solid FDCA from the reaction mixture in a solid/liquid separation step, and providing part of the MY solution resulting from the solid/liquid separation step to the step of combining MFDC with HY. The step of providing part of MY salt solution resulting from the solid/liquid separation step to the step of combining MFDC with HY makes it possible to obtain a stable and economic process which results in an FDCA product with good quality and high yield. 1. Method for manufacturing furan-2 ,5-dicarboxylic acid (FDCA) by converting a furan-2 ,5-dicarboxylate salt (MFDC) into furan-2 ,5-dicarboxylic acid (FDCA) , comprising the steps ofcombining an aqueous solution of MFDC with a concentration of at least 5 wt.% with an inorganic acid (HY), to form a reaction mixture comprising solid FDCA in a concentration of 1-15 wt.% in a solution of a salt resulting from the cation of the furan-2,5-dicarboxylate salt and the anion of the inorganic acid (MY solution),removing solid FDCA from the reaction mixture in a solid/liquid separation step, andproviding part of the MY solution resulting from the solid/liquid separation step to the step of combining MFDC with HY.2. Method according to claim 1 , wherein the salt of furan-2 claim 1 ,5-dicarboxylate is selected from sodium furan-2 claim 1 ,5-dicarboxylate (NaFDC) claim 1 , potassium furan-2 claim 1 ,5-dicarboxylate (KFDC) claim 1 , and ammonium furan-2 claim 1 ,5-dicarboxylate (NH4FDC).3. Method according to claim 1 , wherein the MFDC is provided in the form of an aqueous ...

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Номер записи: 68
19-02-2015 дата публикации

OXIDATION PROCESS TO PRODUCE A CRUDE AND/OR PURIFIED CARBOXYLIC ACID PRODUCT

Номер: US20150051412A1
Автор: Bowers Bradford Russell, Janka Mesfin Ejerssa, Lange David, Morrow Michael C., Parker Kenny Randolph, Partin Lee Reynolds, Shaikh Ashfaq, Sumner Charles
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid. 1. A carboxylic acid composition consisting essentially of:(a) furan-2,5-dicarboxylic acid in an amount greater than 90 weight percent;(b) b* value less than 15; and(c) FFCA in a range of from about 0.1 to about 4.0 weight percent2. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 92 weight percent.3. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.4. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.5. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 94 weight percent.6. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.7. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.8. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 96 weight percent.9. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 10.10. A carboxylic acid composition according to wherein said carboxylic acid composition has a b* value less than 5.11. A carboxylic acid composition according to where said furan-2 claim 1 ,5-dicarboxylic acid is in an amount greater than 98 weight percent. This application is a continuation-in-part of U.S. Non- ...

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Номер записи: 69
03-03-2022 дата публикации

COMPOSITE MATERIAL AND METHOD FOR PRODUCING THE SAME

Номер: US20220064134A1
Автор: CORVAGLIA Stefano Giuseppe, GALLO Nicola, PAPPADA Silvio
Принадлежит:

A composite material, in particular for aeronautical applications, comprising: a first pre-impregnated layer having a resin-based matrix reinforced with fibres to give the first layer predefined mechanical properties; and a second layer of magnetic field intensifier material, superimposed on a face of the first layer and joined to the first layer along that face; the second layer comprises electrically conductive fibres, preferably of carbon, dispersed in the second layer in at least two directions with different orientations and having equivalent electrical resistivity, parallel to the aforementioned face, of less than 600 μΩm, preferably less than 200 μΩm and even more preferably less than 100 μΩm, so as to facilitate localized heating by electromagnetic induction; the first and second layers joined together define a lamina of super-weldable composite material.

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Номер записи: 70
03-03-2022 дата публикации

Method for Preparation of 1,4-Sorbitan in Aqueous Medium

Номер: US20220064135A1
Автор: Jiang Weicheng, Paradies Gesa, Scherer Dieter, Wei Jieping, Wyler Benjamin, Yang Yanling, Zhang Xiaolong, Zhu Reta
Принадлежит:

The invention discloses a method for preparation of 1,4-sorbitan by dehydration of D-sorbitol in aqueous medium, wherein one equivalent of water is removed and a cyclization occurs, followed by a treatment with ethanol and isopropanol.

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Номер записи: 71
25-02-2021 дата публикации

STRONGLY LEWIS ACIDIC METAL-ORGANIC FRAMEWORKS FOR CONTINUOUS FLOW CATALYSIS

Номер: US20210053042A1
Автор: Feng Xuanyu, Ji Pengfei, LIN WENBIN
Принадлежит:

Lewis acidic metal-organic framework (MOF) materials comprising triflate-coordinated metal nodes are described. The materials can be used as heterogenous catalysts in a wide range of organic group transformations, including Diels-Alder reactions, epoxide-ring opening reactions, Friedel-Crafts acylation reactions and alkene hydroalkoxylation reactions. The MOFs can also be prepared with metallated organic bridging ligands to provide heterogenous catalysts for tandem reactions and/or prepared as composites with support particles for use in columns of continuous flow reactor systems. Methods of preparing and using the MOF materials and their composites are also described. 1. A method for preparing a catalyst , said method comprising:{'sub': '2', '(a) providing a parent metal-organic framework (MOF), wherein the parent MOF comprises periodic repeats of a coordination complex comprising (i) an organic bridging ligand and (ii) a metal-containing secondary building unit (SBU), wherein said metal-containing SBU comprises a metal oxo cluster comprising a metal ion M and one or more terminal or bridging OH or OHligands; and'}{'sub': '2', '(b) reacting the parent MOF with a silyl triflate to replace one or more of the one or more terminal or bridging OH or OHligands with a triflate ligand.'}2. The method of claim 1 , wherein the SBU is selected from the group consisting of Zr-oxo cluster claim 1 , a Fe-oxo cluster claim 1 , a Cr-oxo cluster claim 1 , and an A-oxo cluster.3. The method of claim 1 , wherein the organic bridging ligand is substituted with one or more carboxylate claim 1 , pyridine claim 1 , and/or phosphonate moieties.4. The method of claim 3 , wherein the organic bridging ligand is trimesic acid (BTC).5. The method of claim 1 , wherein the parent MOF is provided by contacting a parent precursor MOF with a strong acid claim 1 , wherein the parent precursor MOF comprises periodic repeats of a coordination complex comprising: (i) the organic bridging ligand and (ii ...

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Номер записи: 72
14-02-2019 дата публикации

PROCESSES FOR PREPARING 2,5-FURANDICARBOXYLIC ACID AND ESTERS THEREOF

Номер: US20190047973A1
Автор: Metkar Pranit S., Ozer Ronnie, RAJAGOPALAN BHUMA
Принадлежит:

A process for producing furan dicarboxylic acid or an ester thereof from a feedstock comprising hydroxymethyl furfural (HMF) and humins is disclosed. Humins are a byproduct from reactions forming HMF from sugars and are typically removed from the HMF prior to any further processing. A humins-containing HMF feedstock is utilized to produce furan dicarboxylic acids and ester substantially free from humins. 12-. (canceled)3. A process , comprising:i) oxidizing a feedstock comprising hydroxymethyl furfural and humins in a solvent to produce a mixture comprising crude humins-containing 2,5-furan dicarboxylic acid; andii) filtering the mixture under high temperature to obtain a filtrate comprising 2,5-furan dicarboxylic acid substantially free of humins, wherein the filtration temperature is sufficiently high to keep the 2,5-furan dicarboxylic acid soluble in the solvent.4. The process of claim 3 , wherein the high temperature of the filtering step ii) is in the range of from 50° C. to 200° C.5. The process of claim 3 , further comprising a step iii) crystallizing the 2 claim 3 ,5-furan dicarboxylic acid substantially free of humins to obtain further purified 2 claim 3 ,5-furan dicarboxylic acid.6. The process of claim 3 , wherein the solvent is acetic acid or a mixture of acetic acid and water.714-. (canceled) This application claims benefit of priority of U.S. Provisional Application No. 62/196,808 filed on Jul. 24, 2015, which is incorporated herein by reference in its entirety.The present disclosure is directed towards processes for preparing 2,5-furandicarboxylic acid and esters thereof, especially diesters thereof, from mixtures comprising 5-hydroxymethyl furfural and humins.Poly (trimethylene furandicarboxylate (PTF) is a renewable polyester and can be synthesized via the polycondensation reaction of 2,5-furandicarboxylic acid or 2,5-furandicarboxylic acid diester with 1,3-propane diol. Compared with polyethylene terephthalate (PET), PTF demonstrates improved ...

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Номер записи: 73
22-02-2018 дата публикации

Method for Inhibiting Growth of Ovarian Cancer Cells

Номер: US20180050012A1
Автор: Huang Chun-Chih, TZENG Yew-min, Wu Tsang-Hsien Alexander, YEH CHI-TAI
Принадлежит: NEW BELLUS ENTERPRISES CO., LTD.

The present invention is directed to a method for inhibiting growth of ovarian cancer cells in a subject in need thereof, comprising administering to said subject a composition comprising an effective amount of 4-acetyl-antroquinonol B or a pharmaceutical acceptable salt thereof, and a pharmaceutically acceptable carrier. 1. A method for inhibiting growth of ovarian cancer cells in a subject in need thereof , comprising administering to said subject a composition comprising an effective amount of 4-acetyl-antroquinonol B or a pharmaceutical acceptable salt thereof , and a pharmaceutically acceptable carrier.2. The method of claim 1 , wherein the composition further comprises an anti-cancer drug.3. The method of claim 2 , the anti-cancer drug comprises Fluorouracil claim 2 , Oxaliplatin claim 2 , or a combination of Fluorouracil and Oxaliplatin.4. The method of claim 1 , wherein the composition has the ability of treating or preventing cancer.5Antrodia cinnamomea. The method of claim 1 , wherein the 4-acetyl-antroquinonol B is prepared through extraction of mycelium of with an organic solvent followed by purification via silica gel column chromatography.6. The method of claim 1 , wherein the effective amount of 4-acetyl-antroquinonol B is 0.01-1000 μM.7. The method of claim 1 , wherein the effective amount of 4-acetyl-antroquinonol B is 0.5-50 μM.8. The method of claim 3 , wherein the amount of Fluorouracil is 5-300 mg/mL.9. The method of claim 3 , wherein the amount of Oxaliplatin is 0.5-50 mg/mL.10. The method of claim 3 , wherein the composition prevents the subject from weight loss due to anti-cancer drug intake. The present invention claims foreign priority to Taiwanese patent application No. TW 105126636, filed on Aug. 19, 2016, which is hereby incorporated by reference in its entirety.The present invention is related to a method of treating ovarian cancer by using 4-acetyl-antroquinonol B to inhibit growth of ovarian cancer cells.Cancer, a kind of disease, can ...

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Номер записи: 74
08-05-2014 дата публикации

Method of Synthesizing Low Color Furan Diesters

Номер: US20140128623A1
Автор: Baker, Janka Mesfin Ejerssa, JR. John Dayton, Rollins Stephanie Nicole
Принадлежит: EASTMAN CHEMICAL COMPANY

The present invention relates to a method of synthesizing a low colored furan-2,5-dicarboxylate derivative plasticizer by utilizing purified FDCA (pFDCA), which has very low level 5-formyl furan-2-carboxyic acid (FFCA) and very low level colored bodies, and an alcohol. 1. A method for preparing a furan-2 ,5-dicarboxylate derivative plasticizer , comprising:a) providing a purified furan-2,5-dicarboxylic acid composition; and{'sub': 4', '13, 'b) contacting said purified furan-2,5-dicarboxylic acid composition and an alcohol stream comprising C-Calcohols in the presence of a catalyst to produce a low color furan-2,5-dicarboxylate derivative plasticizer.'}2. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer has an APHA of less than 100.3. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer has a b* value of less than 10.4. The method according to claim 1 , wherein the alcohol stream includes at least one of a Cto Calcohol.5. The method according to claim 4 , wherein the alcohol stream is butanol claim 4 , pentanol claim 4 , hexanol claim 4 , cyclohexanol claim 4 , heptanol claim 4 , 2-ethylhexanol (EH) claim 4 , cyclohexanemethanol claim 4 , isomers of methylcyclohexanemethanol claim 4 , octanol claim 4 , nonanol claim 4 , benzyl alcohol claim 4 , 2-phenyl ethanol claim 4 , decanol or mixtures thereof.6. The method according to claim 1 , wherein the purified furan-2 claim 1 ,5-dicarboxylic acid composition has 5-formyl furan-2-carboxyic acid level of less than about 200 ppm.7. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer is dibutyl furan-2 claim 1 ,5-dicarboxylate claim 1 , dipentyl furan-2 claim 1 ,5-dicarboxylate claim 1 , dihexyl furan-2 claim 1 ,5-dicarboxylate claim 1 , diheptyl furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(2-ethylhexyl)furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(dioctyl)furan-2 claim 1 , ...

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Номер записи: 75
08-05-2014 дата публикации

METHOD OF SYNTHESIZING LOW COLOR FURAN DIESTERS

Номер: US20140128624A1
Автор: Baker, Janka Mesfin Ejerssa, JR. John Dayton, Rollins Stephanie Nicole
Принадлежит: EASTMAN CHEMICAL COMPANY

The present invention relates to a method of making low colored bis(2-ethylhexyl) furan-2,5-dicarboxylate (BEHFD) plasticizer via mild hydrogenation of highly colored BEHFD. 1. A method for preparing a low color furan-2 ,5-dicarboxylate derivative plasticizer , comprising:a) providing a furan-2,5-dicarboxylate derivative; andb) contacting the furan-2,5-dicarboxylate derivative with hydrogen in the presence of a hydrogenation catalyst to thereby produce a low color furan-2,5-dicarboxylate derivative plasticizer.2. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer has an APHA of less than 100.3. The method according to claim 2 , wherein the furan-2 claim 2 ,5-dicarboxylate derivative plasticizer has an APHA of less than 60.4. The method according to claim 3 , wherein the furan-2 claim 3 ,5-dicarboxylate derivative plasticizer has an APHA of less than 40.5. The method according to claim 4 , wherein the furan-2 claim 4 ,5-dicarboxylate derivative plasticizer has an APHA of less than 20.6. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer has a b* value of less than 10.7. The method according to claim 6 , wherein the furan-2 claim 6 ,5-dicarboxylate derivative plasticizer has a b* value of less than 5.8. The method according to claim 1 , wherein the furan-2 claim 1 ,5-dicarboxylate derivative plasticizer is dibutyl furan-2 claim 1 ,5-dicarboxylate claim 1 , dipentyl furan-2 claim 1 ,5-dicarboxylate claim 1 , dihexyl furan-2 claim 1 ,5-dicarboxylate claim 1 , diheptyl furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(2-ethylhexyl) furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(dioctyl) furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(dibenzyl) furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(dinonyl) furan-2 claim 1 ,5-dicarboxylate claim 1 , bis(didecyl) furan-2 claim 1 ,5-dicarboxylate or mixtures thereof.9. The method according to claim 1 , wherein the hydrogenation ...

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Номер записи: 76
23-02-2017 дата публикации

SYNTHESIS OF FDCA AND FDCA PRECURSORS FROM GLUCONIC ACID DERIVATIVES

Номер: US20170050944A1
Автор: Griffin Benjamin M., Kambourakis Spiros
Принадлежит:

The present invention provides methods of method of synthesizing 2,5-furan dicarboxylic acid (FDCA) and FDCA precursor molecules. The methods involve performing a chemical dehydration reaction on a gluconic acid derivative in the presence of a dehydration catalyst. In some embodiments the gluconic acid derivative can be 2-dehydro-3-deoxy gluconic acid (DHG) or an ester thereof, 2-ketogluconic acid (2KGA) or an ester thereof, and 5-ketogluconic acid (5KGA) or an ester thereof. The 2,5-furan dicarboxylic acid precursor molecule is thereby synthesized, which can be converted into FDCA. The chemical dehydration can be performed by a variety of acid basic catalysts. 1. A method of synthesizing a 2 ,5-furan dicarboxylic acid (FDCA) precursor molecule comprising:performing a chemical dehydration reaction on 2-dehydro-3-deoxy gluconic acid (DHG) or an ester thereof, 2-ketogluconic acid (2KGA) or an ester thereof, or 5-ketogluconic acid (5KGA) or an ester thereof, in the presence of a dehydration catalyst;thereby synthesizing the 2,5-furan dicarboxylic acid precursor molecule.2. The method of wherein the dehydration catalyst is an acid catalyst.3. The method of wherein the acid catalyst is a mineral acid.4. The method of wherein the mineral acid is selected from the group consisting of: HSO claim 3 , HCl claim 3 , HClO claim 3 , HBr claim 3 , NbO claim 3 , and HPO.5. The method of wherein the dehydration catalyst is an immobilized catalyst.6. The method of wherein the immobilized catalyst comprises a copolymer of polystyrene and divinylbenzene claim 5 , or zeolite.7. The method of wherein the FDCA precursor is selected from the group consisting of: 2-formyl-5-furan carboxylic acid (FFCA) and 2-hydroxymethyl-5-furan carboxylic acid (HFCA).8. The method of wherein the reaction is performed in a solvent selected from the group consisting of: acetic acid and water claim 7 , or a mixture of acetic acid and water claim 7 , or a mixture of an alcohol and water.9. The method of ...

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Номер записи: 77
15-05-2014 дата публикации

Quinone based nitric oxide donating compounds

Номер: US20140135389A1
Автор: Francesca Benedini, Gael Ronsin, Laura Storoni
Принадлежит: Nicox Sa

The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

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Номер записи: 78
15-05-2014 дата публикации

Method for producing hydride using unsaturated compound having carbon number of 4 as raw material

Номер: US20140135511A1
Автор: Kouta Tanaka, Masaru Utsunomiya, Norikazu Konishi, Yusuke Izawa
Принадлежит: Mitsubishi Chemical Corp

The present invention relates to a method for producing a hydride having a carbon number of 4, comprising contacting, in liquid phase, an unsaturated compound having a carbon number of 4 as a raw material with a solid catalyst obtained by loading a metal element belonging to Groups 9 to 11 of the long periodic table on a support, thereby performing hydrogenation to produce a corresponding hydride having a carbon number of 4, wherein hydrogenation is performed in the presence of, as a solvent, a 1,4-butanediol having a nitrogen component concentration of 1 ppm by weight to 1 wt % in terms of nitrogen atom.

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Номер записи: 79
02-03-2017 дата публикации

N-ARYLAMIDINE-SUBSTITUTED TRIFLUOROETHYL SULFIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES

Номер: US20170057914A1
Автор: ALIG Bernd, Becker Angela, CEREZO-GALVEZ SILVIA, FISCHER Reiner, Goergens Ulrich, Gomibuchi Takuya, HAHN Julia Johanna, ILG Kerstin, ITO Masahito, KOEHLER Adeline, Moradi Wahed Ahmed, Schwarz Hans-Georg, Shibuya Katsuhiko, Shimojo Eiichi, VOERSTE Arnd, Yamazaki Daiei
Принадлежит:

The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) This application is a divisional application of U.S. application Ser. No. 14/366,715 (filed Jun. 19, 2014), which is a §371 National Stage Application of PCT/EP2012/075269 (filed Dec. 12, 2012), which claims priority to EP 11194855.0 (filed Dec. 21, 2011), the contents of each of which are incorporated herein by reference.Field of the InventionThe present invention relates to novel N-arylamidine-substituted trifluoroethyl sulfide derivatives, to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.Description of Related ArtVarious substituted N-arylamidines and their insecticidal and acaricidal action have already been described in the literature in WO 2007/131680.On application, the active compounds already known from the publications mentioned above have disadvantages, be it that they may have no or else only insufficient insecticidal and/or acaricidal activity against animal pests, in particular at relatively low application rates.Accordingly, it is an object of the present invention to provide corresponding N-arylamidine-substituted trifluoroethyl sulfide derivatives which can be employed as insecticides and/or acaricides with satisfactory insecticidal and/or acaricidal activity against animal pests, in particular at relatively low application rates, with high selectivity and improved compatibility in crops of useful plants.The present invention now provides novel compounds of the formula (I)in whichIf appropriate, the compounds of the formula (I) may be present in various polymorphic forms or as mixtures of different polymorphic forms. Both the pure polymorphs and the polymorph mixtures are provided by the invention and can be used according to the invention.The compounds of the formula (I) optionally comprise diastereomers or enantiomers and also rotamers, tautomers and ...

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Номер записи: 80
20-02-2020 дата публикации

PRODUCTION OF 2,5-FURANDICARBOXYLIC ACID

Номер: US20200055832A1
Автор: BISSELINK Roel Johannes Martinus, CROCKATT Marc, Goetheer Earl Lawrence Vincent, LATSUZBAIA Roman, Roelands Cornelis Petrus Marcus
Принадлежит:

The invention is directed to the to the electrochemical preparation of 2,5- furandicarboxylic acid (FDCA) from 5-hydroxymethylfurfural (HMF) by electrochemical oxidation, comprising a first oxidation step of oxidizing HMF to 5-hydroxymethyl-2-furan-carboxylic acid (HMFCA) in an electrochemical cell, subsequently a first isolation step of isolating HMFCA, followed by a second oxidation step of HMFCA to FDCA. 1. A process for electrochemically preparing 5-hydroxymethyl-2-furan-carboxylic acid , said process comprising a first oxidation step of oxidizing 5-hydroxymethylfurfural to 5-hydroxymethyl-2-furan-carboxylic acid in an electrochemical cell , and subsequently a first isolation step of isolating 5-hydroxymethyl-2-furan-carboxylic acid.2. A process for preparing 2 claim 1 ,5-furandicarboxylic acid claim 1 , said process comprising electrochemically preparing 5-hydroxymethyl-2-furan-carboxylic acid from 5-hydroxymethylfurfural in accordance with claim 1 , followed by a second oxidation step of 5-hydroxymethyl-2-furan-carboxylic acid to 2 claim 1 ,5-furandicarboxylic acid.3. The process of claim 1 , wherein the oxidation of 5-hydroxymethylfurfural to 5-hydroxymethyl-2-furan-carboxylic acid in the first oxidation step is carried out in an anode compartment of the electrochemical cell claim 1 , said anode compartment comprising a gold-comprising anode.4. The process of claim 1 , wherein the electrochemical cell comprises an anode compartment and said anode compartment comprises an electrolyte comprising ammonium claim 1 , sodium claim 1 , potassium claim 1 , calcium claim 1 , magnesium claim 1 , perchlorate claim 1 , sulfate claim 1 , hydrogen phosphate claim 1 , a solid polymer electrolyte or a combination thereof.5. The process of claim 1 , wherein the first oxidation step is carried out in a solution having a pH of less than 14.6. The process of claim 1 , wherein a reduction reaction of a bio-based compound is carried out in a cathode compartment of the ...

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Номер записи: 81
05-03-2015 дата публикации

METAL OXIDE-ORGANIC HYBRID MATERIALS FOR HETEROGENEOUS CATALYSIS AND METHODS OF MAKING AND USING THEREOF

Номер: US20150065339A1
Автор: Anastas Paul T., Bloomfield Aaron J., Collom Samuel L., Crabtree Robert H., Sheehan Stafford W.
Принадлежит:

Catalysts prepared from abundant, cost effective metals, such as cobalt, nickel, chromium, manganese, iron, and copper, and containing one or more neutrally charged ligands (e.g., monodentate, bidentate, and/or polydentate ligands) and methods of making and using thereof are described herein. Exemplary ligands include, but are not limited to, phosphine ligands, nitrogen-based ligands, sulfur-based ligands, and/or arsenic-based ligands. In some embodiments, the catalyst is a cobalt-based catalyst or a nickel-based catalyst. The catalysts described herein are stable and active at neutral pH and in a wide range of buffers that are both weak and strong proton acceptors. While its activity is slightly lower than state of the art cobalt-based water oxidation catalysts under some conditions, it is capable of sustaining electrolysis at high applied potentials without a significant degradation in catalytic current. This enhanced robustness gives it an advantage in industrial and large-scale water electrolysis schemes. 1. A heterogeneous catalyst having the chemical formula{'br': None, 'sub': a', 'b', 'c', 'd', '2', 'e, 'MY(CO)O(OH)(HO)'} M is a d-block transition metal;', 'Y is a monodentate ligand, bidentate ligand, polydentate ligand, or combinations thereof;', 'a is any value from about 0 to about 3;', 'b is any value from about 0 to about 3;', 'c is any value from about 1 to about 4; and', 'd is any value from about 0 to about 4; and', 'e is any value from about 0 to about 6., 'wherein'}2. The catalyst of claim 1 , wherein M is selected from the group consisting of Cr claim 1 , Mn claim 1 , Fe claim 1 , Co claim 1 , Ni claim 1 , Cu claim 1 , Rh claim 1 , Ir claim 1 , or combinations thereof.3. The catalyst of claim 1 , wherein M is cobalt.4. The catalyst of claim 1 , wherein M is nickel.5. The catalyst of claim 1 , wherein the M is chromium.6. The catalyst of claim 1 , wherein the M is copper.7. The catalyst claim 1 , wherein the M is iron.8. The catalyst of claim 1 , ...

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Номер записи: 82
05-03-2015 дата публикации

SYNTHETIC PROCESS FOR PREPARATION OF MACROCYCLIC C1-KETO ANALOGS OF HALICHONDRIN B AND INTERMEDIATES USEFUL THEREIN

Номер: US20150065733A1
Автор: BEXRUD Jason A., Gorin Boris, Ngooi Teng Ko, ORPRECIO Ricardo, PAN Ming, Rangwala Huzaifa, Rudolph Alena, SOUZA Fabio E.S.
Принадлежит:

Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed. 136-. (canceled)39. The compound according to claim 37 , wherein{'sup': 10', '11', '12, '(a) R, Ror Ris an alcohol protecting group, a silyl protecting group, or tert-butyldimethyl silyl (TBS); and/or'}{'sup': '13', '(b) Ris ═O; and/or'}{'sup': 9', '8', '8', '9, '(c) Ris I and/or Ris —C(═O)H, or Rand Rtogether form —C(═O)—.'}42. The compound according to claim 37 , wherein Ris —CHOR claim 37 , wherein Ris H or an alcohol protecting group.45. The compound according to claim 43 , wherein R′ is H and R″ is —CHSO—Ar claim 43 , wherein Ar is an aryl group.46. The compound according to claim 43 , wherein R′ is —CHC(═O)—R claim 43 , and wherein Ris H or OR claim 43 , wherein Ris H or a hydrocarbon claim 43 , the hydrocarbon optionally having one or more heteroatoms.49. The process according to claim 48 , wherein the coupling reaction is performed using a base.52. A process for preparation an analog of halichondrin claim 47 , comprising the process as defined in .53. Eribulin mesylate having a purity of more than 95% claim 47 , 96% claim 47 , 97% claim 47 , 98% or 99% claim 47 , as determined by HPLC.56. The compound according to claim 40 , wherein Ris —CHOR claim 40 , wherein Ris H or an alcohol protecting group. This application claims the benefit of and priority to U.S. Provisional Application Nos. 61/618,004 filed Mar. 30, 2012, entitled MACROCYCLIC ANALOGS AND METHODS FOR THEIR PREPARATION, and 61/647,127 filed May 15, 2012, entitled SYNTHETIC PROCESS FOR PREPARATION OF ...

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Номер записи: 83
05-03-2015 дата публикации

METHOD FOR PRODUCING PURIFIED DIALKYL-FURAN-2,5-DICARBOXYLATE BY PHYSICAL SEPARATION AND SOLID LIQUID SEPARATION

Номер: US20150065735A1
Автор: Janka Mesfin Ejerssa, Parker Kenny Randolph, Parton Lee Raynolds, Shaikh Ashfaq
Принадлежит:

A process to produce a purified dimethyl-furan-2,5-dicarboxylate (DMFD) by feeding furan dicarboxylic acid and methanol to an esterification zone to generate a crude diester composition, and purifying the crude diester composition with a physical separation process followed by crystallization, solid liquid separation, and optionally drying to produce a purified DMFD composition. A portion of the stream generated by solid liquid separation can be dissolved and subjected to crystallization and solid liquid separation repeatedly. The process is useful to produce a purified DMFD composition having a low b*, at least 98 wt. % DAFD solids, and a low concentration of 5-(methoxycarbonyl)furan-2-carboxylic acid (MCFC) and methyl 5-formylfuran-2-carboxylate (MFFC). 1. A dialkyl furan dicarboxylate (DAFD) composition , comprising:(i) at least 98 wt. % solids based on the weight of the composition, said solids comprising DAFD in an amount of greater than 98 wt. % based on the weight of the solids,(ii) a b* of 5 or less,(iii) not more than 3 wt. % 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC),(iv) not more than 3 wt. % alkyl 5-formylfuran-2-carboxylate (AFFC), and(v) not more than 1 wt. % FDCA.2. The DAFD composition of claim 1 , wherein the DAFD compounds are dimethyl furan dicarboxylate (DMFD) claim 1 , said DAFD composition further comprising:(i) at least 98 wt. % solids based on the weight of the composition, said solids comprising DMFD in an amount of greater than 98 wt. % based on the weight of the solids.3. The DAFD composition of claim 2 , comprising:(i) not more than 0.3 wt. % 5-(methoxycarbonyl)furan-2-carboxylic acid (MCFC), and(ii) not more than 0.8 wt. % methyl 5-formylfuran-2-carboxylate (MFFC).4. The DAFD composition of claim 1 , wherein said DAFD composition comprises:(i) not more than 1000 ppm MCFC, and(ii) not more than 1000 ppm MFFC. This application is a divisional of U.S. application Ser. No. 13/530,765, filed Jun. 22, 2012. The entire disclosure of the ...

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Номер записи: 84
22-05-2014 дата публикации

Process for the preparation of (2r,3s)-2-(hydroxymethyl)-5-methoxytetrahydrofuran-3-ol and acetylated derivatives thereof, free of pyranose compounds

Номер: US20140142296A1
Автор: Albercht Zumbrunn, Xing FU
Принадлежит: JOHNSON MATTHEY PLC

The invention provides methyl-2-deoxyriboside containing at most 5 wt % of methyl-2-deoxyribopyranoside, based on the combined weight of methyl-2-deoxyriboside and methyl-2-deoxyribopyranoside.

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Номер записи: 85
22-05-2014 дата публикации

PROCESS FOR PRODUCING DRY PURIFIED FURAN-2,5-DICARBOXYLIC ACID WITH OXIDATION OFF-GAS TREATMENT

Номер: US20140142326A1
Автор: Janka Mesfin Ejerssa, Parker Kenny Randolph, Partin Lee Reynolds, Shaikh Ashfaq Shahanawaz
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is a process for producing a dry, purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). Also disclosed is a method for treating an oxidation off-gas stream from such a process. The method features solvent as well as energy recovery from the off-gas stream. 1. A method for treating an off-gas stream from a process for producing a carboxylic acid product comprising furan-2 ,5-dicarboxylic acid , the method comprising:(a) providing an off-gas stream comprising an organic acid solvent vapor, water vapor, and an inert gas from a primary oxidation zone of a process for producing a carboxylic acid product comprising furan-2,5-dicarboxylic acid;(b) passing the off-gas stream to a solvent recovery zone to condense and separate at least a portion of the organic acid solvent vapor and the water vapor to obtain a water-rich stream, a solvent-rich stream, and a high-energy inert gas stream;(c) passing the high-energy inert gas stream to a power recovery zone to convert the high-energy inert gas stream to a low-energy inert gas stream and to generate an electrical power stream;(d) passing the electrical power stream to a compression zone to convert a low-pressure gas stream comprising oxygen into a high-pressure gas stream comprising oxygen;(e) passing the low-energy inert gas stream and a stream comprising an oxidizable fuel and oxygen to a thermal oxidation zone to combust at least a portion of organic compounds in the low-energy inert gas stream and generate a thermal oxidation gas stream; and(f) passing the thermal oxidation gas stream to a scrubbing zone to generate a treated off-gas stream and a liquid scrubbing effluent stream comprising water.2. The method according to claim 1 , wherein the solvent recovery zone comprises a distillation column.3. The method according to claim 1 , wherein the solvent-rich stream comprises from 4 to 25% by weight of water.4. The method according to claim 1 , wherein the water-rich stream comprises at ...

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Номер записи: 86
22-05-2014 дата публикации

Process for producing dry purified furan-2,5-dicarboxylic acid with oxidation off-gas treatment

Номер: US20140142327A1
Автор: Ashfaq Shahanawaz Shaikh, Kenny Randolph Parker, Lee Reynolds Partin, Mesfin Ejerssa Janka
Принадлежит: Eastman Chemical Co

Disclosed is a process for producing a dry, purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). Also disclosed is a method for treating an oxidation off-gas stream from such a process. The method features solvent as well as energy recovery from the off-gas stream.

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Номер записи: 87
22-05-2014 дата публикации

OXIDATIVE PURIFICATION METHOD FOR PRODUCING PURIFIED DRY FURAN-2,5-DICARBOXYLIC ACID

Номер: US20140142328A1
Автор: Janka Mesfin Ejerssa, Parker Kenny R., Partin Lee R., Shaikh Ashfaq
Принадлежит: EASTMAN CHEMICAL COMPANY

Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising FDCA, removing impurities from a crude carboxylic acid slurry via oxidative purification in a low temperature post-oxidation zone to form a low impurity slurry stream. The low impurity slurry stream is further treated in a high temperature post oxidation zone to produce a secondary oxidation slurry stream which is routed to a crystallization zone to from a crystallized slurry stream. 1. A process to produce a purified slurry stream comprising furan-2 ,5-dicarboxylic acid (FDCA) , said process comprising:(a) oxidizing in primary oxidation zone an oxidizable compound in an oxidizable raw material stream in the presence of a solvent stream, an oxidizing gas stream, and a catalyst system, wherein said oxidizable raw material stream comprises at least one compound selected from the group consisting of 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural where R=alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R′OCH2-furfural, where R′=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R″-furfural, where R″=alkyl, cycloalkyl and aryl), mixed feedstocks of 5-HMF and 5-HMF esters, mixed feedstocks of 5-HMF and 5-HMF ethers, and mixed feedstocks of 5-HMF and 5-alkyl furfurals to produce a crude carboxylic acid composition comprising furan-2,5-dicarboxylic acid (FDCA);(b) routing said crude carboxylic acid composition to a low temperature post oxidation zone to form a low impurity stream; wherein said low impurity stream comprises FDCA; wherein said FFCA in said low impurity stream is less than 2000 ppm;(c) routing said low impurity slurry stream to a high temperature post oxidation zone to form secondary oxidation slurry stream; wherein said secondary oxidation slurry stream comprises FDCA; wherein said ...

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Номер записи: 88
10-03-2016 дата публикации

2,3-Fluorinated Glycosides as Neuraminidase Inhibitors and Their Use as Anti-Virals

Номер: US20160068501A1
Автор: Kim Jin Hyo, Watts Andrew Graham, Wennekes Tom, Withers Stephen
Принадлежит:

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza. 140.-. (canceled)42. (canceled) This application is a divisional of U.S. application Ser. No. 14/330,855 filed on Jul. 14, 2014, which is a continuation of U.S. application Ser. No. 13/382,284 filed on Mar. 26, 2012, now U.S. Pat. No. 8,815,941, which is a National Stage Entry of PCT/CA2010/001063 filed on Jul. 15, 2010, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/213,786 entitled “NEURAMIDINASE INHIBITORS: COMPOSITIONS AND METHOD OF USE FOR THE TREATMENT OF INFLUENZA” filed on Jul. 15, 2009, the disclosures of each of which are incorporated herein by reference in their entirety.This invention relates to therapeutics, their uses and methods for the treatment or prophylaxis of viral infection. In particular the invention relates to compounds, compositions, therapies, and methods of treatment for viral infections such as influenza.Infection and invasion by influenza viruses requires the intermediacy of sialic acid residues on the surface of the host cell. Sialic acid and neuraminic acid are used interchangeably. Similarly, sialidase and neuraminidase are used interchangeably. Initial attachment of the virus to the host cell occurs via the binding of the virus to these sialic acids (charged, 9-carbon sugars) through the hemagglutinin protein of the virus. Once inside the cell the virus replicates by taking advantage of the host cellular machinery. However, in order to remain optimally infective, the virus has evolved a neuraminidase that cuts off the sialic acid from the host cell surface to assist the virus in escaping the host cell to infect other cells. Failure to cut off the sialic acid from the host cell surface, results in ...

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Номер записи: 89
08-03-2018 дата публикации

RUTHENIUM POLYMERISATION CATALYSTS

Номер: US20180065914A1
Автор: Cazin Catherine
Принадлежит:

Cis and trans ruthenium complexes that can be used as catalysts for ring opening metathesis polymerisation (ROMP) are described. The complexes are generally square pyramidal in nature, having two anionic ligands X. Corresponding cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand are also described. Polymers such as polydicyclopentadiene (PDCPD) can be prepared using the catalysts. 3. The method according to wherein the group A is an N-heterocyclic carbene.4. The method according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates.5. The method according to wherein the groups Rand Rare H and aryl.6. The method according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.8. The method according to wherein the anionic ligands X are independently selected from the group consisting pivalate claim 1 , trifluoroacetate claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , phenylacetate claim 1 , and pseudo-halogen.10. The method according to wherein the groups Rand Rare fused together to form a ring that may be substituted or unsubstituted claim 9 , saturated or unsaturated and may be fused to a further ring.11. The method according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.12. The method according to wherein the group A is an N-heterocyclic carbene.14. The method according to wherein Rand Rare aryl.15. The method according to wherein Rand Rare phenyl.16. The method according to wherein Ris selected from the group consisting of substituted or unsubstituted primary alkyl and substituted or unsubstituted aryl.16. The method according to wherein Ris methyl claim 9 , ethyl or phenyl.17. The method of claim 1 , further ...

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Номер записи: 90
08-03-2018 дата публикации

SUBSTITUTED CYCLIC ETHER POLYMERS AND CONJUGATES AND USES THEREOF

Номер: US20180066081A1
Автор: PESAVENTO Russell P.
Принадлежит:

Disclosed herein are substituted cyclic ether monomers, polymers, and drug conjugates thereof, which are useful for the treatment of diseases and conditions of the oral cavity. In particular, disclosed herein are monomers of Formula (I), polymers of Formula (II), drug conjugates of the monomers and polymers, and pharmaceutically acceptable salts and solvates of each: 2. The polymer of claim 1 , further comprising a metal cation complexed to at least one heteroatom of the polymer.34-. (canceled)5. The polymer of claim 1 , wherein m is 1.68-. (canceled)9. The polymer of claim 1 , wherein m is 0.1011-. (canceled)12. The polymer of claim 1 , wherein q is 0.1321-. (canceled)22. The polymer of claim 1 , wherein q is 1.2352-. (canceled)54. The polymer of claim 1 , wherein p+r is at least 10.5556-. (canceled)58. The polymer of claim 1 , further comprising at least one monomer selected from the group consisting of ethylene claim 1 , styrene claim 1 , (Calkyl)acrylamide claim 1 , (Calkyl)acrylate claim 1 , (Calkyl)acrylic acid.59. (canceled)61. The monomer of further comprising a metal cation complexed to at least one heteroatom of the monomer.6286-. (canceled)88. A drug conjugate claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , comprising a therapeutic agent and the polymer of ; wherein the therapeutic agent and monomer or polymer are attached through a linking group selected from the group consisting of an ester linkage claim 1 , a thioester linkage claim 1 , an amide linkage claim 1 , a carbamate linkage claim 1 , a carbonate linkage claim 1 , and a metal ligand bond claim 1 , andthe linking group is formed from the Z group of the monomer or polymer, and a reactive group on the therapeutic agent, such that:(i) Z comprises a hydroxyl group, a thiol group, or an amino group, and the reactive group comprises a carboxylic acid or an activated carboxylic acid; or(ii) Z comprises a carboxylic acid or an activated carboxylic acid, and the reactive group comprises ...

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Номер записи: 91
09-03-2017 дата публикации

Crystalline derivatives of (S)-1-((2R,3R,4S,5S)-5-allyl-3-methoxy-4-(tosylmethyl)tetrahydrofuran-2-YL)-3-aminopropan-2-ol

Номер: US20170066735A1
Автор: ORPRECIO Ricardo, PAN Ming, SOUZA Fabio E.S.
Принадлежит: Alphora Research Inc.

Disclosed are salts of a compound of formula 1, as shown below, where R, R, R, R′ R, Rand Rare as described herein. Also, disclosed is a process for the preparation of the salts of the compounds of formula 1, and intermediates used therein. The salts of the compound of formula 1 can be useful for preparation of halichondrin analogs such as eribulin. 3. The compound according to claim 1 , wherein Ris CH—CH═CH claim 1 , —CH—CH═CH—CH claim 1 , or —CH—CH═C(CH).4. The compound according to claim 1 , wherein Ris —CH—CH═CH.5. The compound according to claim 1 , wherein Ris H claim 1 , a silyl group claim 1 , an acyl group or an alkoxycarbonyl group.6. The compound according to claim 1 , wherein Rand Reach independently is H claim 1 , allyl claim 1 , benzyl or a substituted benzyl group.7. The compound according to claim 1 , wherein one of Rand Ris H and the other is —CHSO—Ar.8. The compound according to claim 1 , wherein one of Rand Ris H and the other is —CHSO—Ar claim 1 , and the carbon to which they are attached has the S-configuration.9. The compound according to claim 1 , wherein Ris a Calkyl group.10. The compound according to claim 1 , wherein Ris methyl.11. The compound according to claim 1 , wherein the salt formed is a hydrochloric acid salt claim 1 , sulfuric acid salt claim 1 , citrate salt claim 1 , hydrobromic acid salt claim 1 , hydroiodic acid salt claim 1 , nitric acid salt claim 1 , bisulfate salt claim 1 , phosphoric acid salt claim 1 , isonicotinic acid salt claim 1 , acetic acid salt claim 1 , lactic acid salt claim 1 , salicic acid salt claim 1 , tartaric acid salt claim 1 , pantotenic acid salt claim 1 , ascorbic acid salt claim 1 , succinic acid salt claim 1 , maleic acid salt claim 1 , fumaric acid salt claim 1 , gluconic acid salt claim 1 , saccharinic acid salt claim 1 , formic acid salt claim 1 , benzoic acid salt claim 1 , glutaminic acid salt claim 1 , methanesulfonic acid salt (also referred to as mesylic acid salt) claim 1 , ethanesulfonic ...

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Номер записи: 92
11-03-2021 дата публикации

Method for Purifying and Removing Color of FDCA

Номер: US20210070722A1
Автор: CROCKATT Marc, Geers Leonard Ferdinand Gerard, ROA ENGEL Carol Andrea, Van der Meer Johannes
Принадлежит:

The invention is based on the finding that when conducting crystallization of FDCA at high temperatures, the formation of significant amounts of colored byproduct can be reduced or even avoided when the FDCA mixture is kept at temperatures above 100° C. for less than 15 minutes. This is achieved by conducting the crystallization process in a continuous reactor. Accordingly, the method comprises the steps of feeding a mixture comprising undissolved FDCA and a solvent to a reactor; and dissolving FDCA by superheating the mixture in the reactor to a temperature of at least 130° C.; and crystallizing FDCA by cooling the mixture in the reactor, wherein the reactor is a continuous reactor and the residence time in the reactor zone wherein the FDCA mixture has a temperature above 100° C. is less than 15 minutes. 1. A method for purifying 2 ,5-furandicarboxylic acid (“FDCA”) comprising the steps offeeding a mixture comprising undissolved FDCA and a solvent to a reactor; anddissolving FDCA by superheating the mixture in the reactor; andcrystallizing FDCA from the mixture by cooling;wherein the reactor is a continuous reactor comprising a reactor zone having a temperature above 100° C.; and wherein the residence time in the reactor zone having a temperature above 100° C. is less than 15 minutes.2. A method for reducing the color of FDCA crystals comprising the steps ofoptionally degassing a solvent; andpreparing a mixture by mixing colored FDCA crystals with the solvent; andfeeding the mixture comprising FDCA crystals to a reactor; anddissolving FDCA by superheating the mixture in the reactor; andcrystallizing FDCA from the mixture by cooling,wherein the reactor is a continuous reactor comprising a reactor zone having a temperature above 100° C.; and wherein the residence time in the reactor zone having a temperature above 100° C. is less than 15 minutes.3. The method according to claim 1 , wherein superheating is conducted under anaerobic conditions.4. The method according ...

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Номер записи: 93
12-03-2015 дата публикации

Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives and intermediates useful thereof

Номер: US20150073157A1
Автор: Boris Gorin, Fabio E.S. Souza, Jason A. BEXRUD, Ricardo Orprecio
Принадлежит: Alphora Research Inc

Discloses is a process for preparation of a compound of formula 7, or a derivative thereof, wherein PG 1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 7 can be useful in the preparation of halinchondrin analogs such as Eribulin.

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Номер записи: 94
17-03-2016 дата публикации

Low-Toxicity Olefinic Ester Compositions and Methods of Using the Same

Номер: US20160075631A1
Автор: DANTALE Shubhada, Erhan Selim, Ngantung Frederyk
Принадлежит: ELEVANCE RENEWABLE SCIENCES, INC.

Compositions including certain olefinic ester compounds are generally disclosed. In some embodiments, such compositions are compositions having low toxicity, such as low aquatic toxicity. Therefore, in some embodiments, such compositions can be suitable used as solvents or as part of a solvent system for applications where low toxicity is desirable. Such uses include, but are not limited to, cleaning applications on or near waterways, use in oil or gas recovery, and the like. In some other embodiments, such compositions are treatment fluids for oil wells, and can therefore be introduced into an oil well to remove buildup and other deposits. In some embodiments, the olefinic ester compounds are derived from a natural oil or a natural oil derivative. 2. The compound of claim 1 , wherein Ris Calkenyl claim 1 , which is optionally substituted.3. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH.3. (canceled)4. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH claim 1 , —(CH)—CH═CH—CH—CH—CH claim 1 , or —(CH)—CH═CH.5. The compound of claim 4 , wherein Ris —(CH)—CH═CH—CH—CH═CH.6. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH claim 1 , —(CH)—CH═CH—CH—CH—CH—CH claim 1 , or —(CH)—CH═CH—CH.7. The compound of claim 6 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH.8. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH—CH claim 1 , —(CH)—CH═CH—(CH)—CH claim 1 , or —(CH)—CH═CH—CH—CH.9. The compound of claim 8 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH—CH.10. The compound of claim 1 , wherein Ris -G-R.11. The compound of claim 1 , wherein Ris R.12. (canceled)13. The compound of claim 10 , wherein Gis —CH— or —CH—CH.14. (canceled)15. (canceled)16. The compound of claim 11 , wherein Ris Ccycloalkyl claim 11 , which is optionally substituted.17. (canceled)18. (canceled)19. The compound of claim 16 , wherein Ris cyclopentyl claim 16 , cyclohexyl claim 16 , norbornyl claim 16 , or adamantyl.20. The compound of claim 19 , wherein Ris cyclohexyl.21. The compound ...

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Номер записи: 95
17-03-2016 дата публикации

TETRAHYDROFURAN DERIVATIVES AND USE THEREOF AS PLASTICIZERS

Номер: US20160075671A1
Автор: Bohn Martin A., Breitscheidel Boris, Kindler Alois, LANK Benoit, Wagner Jochen
Принадлежит:

The invention relates to tetrahydrofuran derivatives of general formula (I), wherein X stands for *—(C═O)—O—, *—(CH2)n-O—, or *—(CH2)n-O—(C═O)—, wherein * represents the point of bonding to the tetrahydrofuran ring and n has the value 0, 1, or 2; and R1 and R2 are selected independently of each other from among C4-C5 alkyl and C5-C6 cycloalkyl, wherein the cycloalkyl groups are unsubstituted or can be substituted by at least one C1-C10 alkyl group, a plasticizer composition that contains said tetrahydrofuran derivatives, molding masses that contain a thermoplastic polymer or an elastomer and such a tetrahydrofuran derivative. The invention further relates to a method for producing said tetrahydrofuran derivatives, and to the use of said tetrahydrofuran derivatives 2. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , Rand Rare independently selected from an unbranched or branched C-alkyl moiety.3. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , Rand Rare independently selected from n-butyl or isobutyl.4. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , both of the groups X are *—(C═O)—O—.5. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is a plasticizer for a thermoplastic polymer which comprises polyvinyl chloride or consists of polyvinyl chloride.6. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is a plasticizer for an elastomer which comprises a natural and/or synthetic rubber or consists of a natural and/or synthetic rubber.7. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is plastisol.8. The polymer or elastomer ...

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Номер записи: 96
17-03-2016 дата публикации

PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF FURAN-2,5-DICARBOXYLIC ACID OR DERIVATIVES THEREOF

Номер: US20160075672A1
Автор: Raaijmakers Henricus Wilhelmus Carolina, VAN DER KLIS Frits, Van Es Daniël Stephan, Van Haveren Jacobus
Принадлежит:

Disclosed is a method of making 5-formyl-2-furoic acid and furan-2,5-dicarboxylic acid. The method involves the use of 5-keto-aldonic acids as intermediates, as these can be subjected to ring formation by a cyclodehydration reaction under mild conditions. The 5-formyl-2-furoic acid or carboxylic derivative thereof is subjected to oxidation so as to form furan-2,5-dicarboxylic acid. The 5-keto-aldonic acid intermediates can be obtained by isomerization of uronic acids which can be obtained from sugar beet pulp, chicory pulp, fruit peals including orange peels, or non-terrestrial sources like seaweeds. A preferred source is sugar beet pulp. 1. A process for the production of furan-2 ,5-dicarboxylic acid , or a carboxylic derivative thereof , comprising making 5-formyl-2-furoic acid , or a carboxylic derivative thereof , by a method comprising the steps of (i) providing an uronic acid; (ii) subjecting the uronic acid to isomerization so as to form the corresponding 5-keto-aldonic acid; (iii) subjecting said 5-keto-aldonic acid to cyclodehydration so as to produce 5-formyl-2-furoic acid or a carboxylic derivative thereof , and subjecting the 5-formyl-2-furoic acid , or the carboxylic derivative thereof , to oxidation so as to form furan-2 ,5-dicarboxylic acid , or a carboxylic derivative thereof.2. A process according to claim 1 , wherein the oxidation is conducted by subjecting the 5-formyl-2-furoic acid or carboxylic derivative thereof to molecular oxygen under the influence of a supported noble metal catalyst claim 1 , preferably selected from the group consisting of gold claim 1 , platinum claim 1 , ruthenium and palladium.3. A process according to claim 2 , wherein the oxidation is conducted in the presence of a base.4. A process according to any one of the preceding claims claim 2 , wherein the catalyst support is carbon.5. A process according to any one of the preceding claims claim 2 , wherein the uronic acid is obtained from bio-based pectins or biobased ...

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Номер записи: 97
16-03-2017 дата публикации

POTENT INHIBITORS OF HUMAN CARBONIC ANHYDRASE II AND BOVINE CARBONIC ANHYDRASE II AND THEIR MECHANISM OF ACTION

Номер: US20170073306A1
Автор: Bhatti Aamer Saeed, Choudhary Muhammad Iqbal, Khan Ajmal, Rahman Atta-ur-, SALEEM Muhammad, Wahab Atia-tul
Принадлежит:

Inhibitors of carbonic anhydrase-II derived from sulfanilamide are reported. 1. A compound with inhibitory activity against carbonic anhydrase-II enzyme selected from the group consisting of:N-(4-Sulfamoylphenylcarbamothioyl)benzamide;4-Chloro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;4-Methyl-N-(4-sulfamoylphenylcarbamothioyl)benzamide;4-Nitro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3-Chloro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3-Nitro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;2-Nitro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;2-Phenyl-N-(4-sulfamoylphenylcarbamothioyl)acetamide;2-Methyl-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3-Methyl-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3-Methoxy-N-(4-sulfamoylphenylcarbamothioyl)benzamide;4-Chloro-2-nitro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;4-Fluoro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3,4,5-Trimethoxy-N-(4-sulfamoylphenylcarbamothioyl)benzamide;2-Chloro-4-nitro-N-(4-sulfamoylphenylcarbamothioyl)benzamide;3,5-Dimethoxy-N-(4-sulfamoylphenylcarbamothioyl)benzamide;N-(4-Sulfamoylphenylcarbamothioyl)tetrahydrofuran-2-carboxamide;2-Phenyl-N-(4-sulfamoylphenylcarbamothioyl)butanamide; and2,4-Dichloro-N-(4(4-sulfamoylphenylcarbamothioyl)benzamide.2. The compound of claim 1 , wherein the compound is derived from a bovine source or manufactured by a recombinant process.3. (canceled) Mechanism based high throughput calorimetric method is a significant procedure for the characterization of the enzymes reaction, and origin of their catalysis in bio-industry. Enzyme inhibition defines, “the interactions of enzyme-substrate or enzyme-inhibitor or both in the moiety of active site”. In recent years, application of enzymes their inhibition have made tremendous progress in the field of healthcare, pharmaceutical, bio-industries, environment, and biochemical enzyme chip industries. Calorimetric enzyme technology has given a new way of drug discovery. Every year new enzyme inhibitors are discovered as ...

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Номер записи: 98
16-03-2017 дата публикации

CATALYTIC CARBONYLATION CATALYSTS AND METHODS

Номер: US20170073463A1
Автор: Allen Scott D., Coates Geoff, Farmer Jay J., Lee Han
Принадлежит: NOVOMER, INC.

In one aspect, the present invention provides catalysts for the carbonylation of heterocycles. The inventive catalysts feature metal-ligand complexes having cationic functional groups tethered to the ligand, wherein the tethered cationic groups are associated with anionic metal carbonyl species. The invention also provides methods of using the inventive catalysts to affect the ring opening carbonylation of epoxides. 1. A catalyst for the carbonylation of heterocycles comprising the combination of:i) one or more cationic functional moieties, where each cationic functional moiety comprises a linker and 1 to 4 cationic functional groups;ii) one or more ligands to which at least one cationic functional moiety is covalently tethered wherein the one or more ligand(s) are coordinated to one or two metal atoms; andiii) at least one anionic metal carbonyl species associated with a cation present on the metal complex.2. The catalyst of claim 1 , wherein the one or more ligands to which at least one cationic functional moiety is covalently tethered is selected from the group consisting of porphryin ligands and salen ligands.3. The catalyst of claim 2 , wherein catalyst comprises a salen or porphyrin complex of a metal selected from the group consisting of: Zn(II) claim 2 , Cu(II) claim 2 , Mn(II) claim 2 , Co(II) claim 2 , Ru(II) claim 2 , Fe(II) claim 2 , Co(II) claim 2 , Rh(II) claim 2 , Ni(II) claim 2 , Pd(II) claim 2 , Mg(II) claim 2 , Al(III) claim 2 , Cr(III) claim 2 , Cr(IV) claim 2 , Ti(IV) claim 2 , Fe(III) claim 2 , Co(III) claim 2 , Ti(III) claim 2 , In(III) claim 2 , Ga(III) claim 2 , Mn(III).4. The catalyst of claim 2 , wherein the catalyst comprises a salen or porphyrin complex of aluminum.5. The catalyst of claim 2 , wherein the catalyst comprises a salen or porphyrin complex of chromium.6. The catalyst of claim 1 , wherein the one or more cationic functional groups comprise onium salts.7. The catalyst of claim 1 , wherein the onium salts comprise at least one ...

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Номер записи: 99
24-03-2022 дата публикации

METHOD FOR THE IN VIVO SYNTHESIS OF 4-HYDROXYMETHYLFURFURAL AND DERIVATIVES THEREOF

Номер: US20220090153A1
Автор: ALEXANDRINO Paulo Moises Raduan, GOUVEA Iuri Estrada
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The present disclosure provides recombinant microorganisms and methods for the production of 4-HMF, 2,4-furandimethanol, furan-2,4-dicarbaldehyde, 4-(hydroxymethyl)furoic acid, 2-formylfuran-4-carboxylate, 4-formylfuran-2-carboxylate, and/or 2,4-FDCA from a carbon source. The method provides for engineered microorganisms that express endogenous and/or exogenous nucleic acid molecules that catalyze the conversion of a carbon source into 4-HMF, 2,4-furandimethanol, furan-2,4-dicarbaldehyde, 4-(hydroxymethyl)furoic acid, 2-formylfuran-4-carboxylate, 4-formylfuran-2-carboxylate, and/or 2,4-FDCA. The disclosure further provides methods of producing polymers derived from 4-HMF, 2,4-furandimethanol, furan-2,4-dicarbaldehyde, 4-(hydroxymethyl)furoic acid, 2-formylfuran-4-carboxylate, 4-formylfuran-2-carboxylate, and/or 2,4-FDCA. 175-. (canceled)76. A recombinant microorganism capable of producing 4-(hydroxymethyl)furoic acid from a feedstock comprising a carbon source , wherein the recombinant microorganism expresses the following:(a) endogenous or exogenous nucleic acid molecules encoding enzymes capable of converting a carbon source to glyceraldehyde 3-phosphate (G3P);(b) at least one endogenous or exogenous nucleic acid molecule encoding a (5-formylfuran-3-yl)methyl phosphate synthase that catalyzes the conversion of G3P from (a) to (5-formylfuran-3-yl)methyl phosphate;(c) at least one endogenous or exogenous nucleic acid molecule encoding a phosphatase that catalyzes the conversion of (5-formylfuran-3-yl)methyl phosphate from (b) to 4-hydroxymethylfurfural (4-HMF); and(d) at least one endogenous or exogenous nucleic acid molecule encoding a dehydrogenase, an oxidase, or a peroxygenase that catalyzes the conversion of 4-HMF from (c) to 4-(hydroxymethyl)furoic acid77. The recombinant microorganism of claim 76 , wherein the carbon source comprises a hexose claim 76 , a pentose claim 76 , glycerol claim 76 , CO claim 76 , sucroses or combinations thereof.78. The recombinant ...

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Номер записи: 100