ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ АНТАГОНИСТОВ CCR2B

Изобретение относится к новым соединениям общей формулы (I) или к их фармацевтически приемлемым солям, обладающим CCR2B антагонистической активностью, и к фармацевтической композиции на их основе. ! , ! где Р представляет собой фенил, возможно замещенный 1 или 2 заместителями, независимо выбранными из галогена, С1-4алкила, циано, трифторметила, С1-4алкокси и трифторметилтио, a R2 имеет значения, указанные в формуле изобретения. 2 н. и 14 з.п. ф-лы.

СПОСОБ ПОЛУЧЕНИЯ ВТОРИЧНЫХ АМИДОВ ПУТЕМ КАРБОНИЛИРОВАНИЯ СООТВЕТСТВУЮЩИХ ТРЕТИЧНЫХ АМИНОВ

... 1. Способ получения вторичного амида следующей формулыгде Rпредставляет ароматическую группу неразветвленную либо разветвленную алифатическую углеродную цепь, содержащую, по меньшей мере, один атом углерода, которая может быть замещенной либо незамещенной;Rи Rпредставляют (независимо друг от друга) ароматическую группу или неразветвленную либо разветвленную алифатическую углеродную цепь, содержащую, по меньшей мере, один атом углерода, которая может быть замещенной либо незамещенной, или же Rи Rобразуют циклическую структуру, содержащую амидный азот;который включает стадию карбонилирования третичного амина формулыс помощью монооксида углерода в реакционной смеси в присутствии катализатора, содержащего палладий, и в присутствии промотора, содержащего галоген, который существенно не поглощается в реакционной смеси.2. Способ по п.1, в котором реакционная смесь содержит менее чем 5000 частей на миллион (ppm), предпочтительно менее 3000 ppm, более предпочтительно менее 1500 ppm, еще более предпочтительно ...

Способ получения пиперазинсодержащих углеводородов или их кислотно-аддитивных солей

Изобретение касается производных пиперазина и, в частности, способа получения пиперазинсодержащих углеводородов (ПУВ) общей формулы М - Z - М, где М - группа - (CH2)M- CR3R4- (CH2)N- C6H3R1R2 R1и R2, одинаковые или различные, - Н, СН3, С1-С4-алкоксил, C, BR, F, - CF3, ацетоксигруппа R3- H или OH R4=H или (R4+R3) - кислород, если M=1 и N=0 M и N означают 0,1,2, причем (M+N)≠3 Z - -K-CR6R7- X - CR8R9-K- R6-R9, одинаковые или различные, - H или CH3, или R6и R7и/или R8и R9- кислород X - C1-C2- алкилен (он может быть замещен - OH) K - группа - @ А- -СН2- или - CH2-CH2- R5-H или 2-4 метильные группы у атомов углерода пиперазинового кольца, или их кислотно-аддитивных солей, обладающих антиаллергической и противовоспалительной активностью, которые могут найти применение в медицине. Цель изобретения - создание новых более активных веществ указанного класса. Синтез ПУВ ведут реакцией соединения формулы H - Z - H и соединения формулы M - Y, где Z, M - см.выше Y - галоген, взятых в соотношении 1:(2 ...

Biphenylderivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel

Verfahren zur Herstellung von als Psychotherapeutica geeigneten basischen Fluorenverbindungen

COLOUR PHOTOGRAPHIC MATERIALS CONTAINING AGENTS FOR PREVENTING DYE IMAGES FROM FADING

New derivatives of quinoline and their preparation.

Process for the preparation of new amines.

VERFAHREN ZUR HERSTELLUNG VON NEUEN PIPERAZINDERIVATEN UND DEREN SALZEN

PROCEDURE FOR THE PRODUCTION OF NEW PIPERAZINDERIVATEN AND OF ENANTIOMEREN OR DIASTEREOMEREN OF IT

PROCEDURE FOR THE PRODUCTION OF NEW PYRIDAZINDERIVATE

PROCEDURE FOR THE PRODUCTION OF NEW POLYCYCLO ALIPHATIC DIAMINES

PROCEDURE FOR THE PRODUCTION OF NEW POLYCYCLO ALIPHATIC DIAMINES

UNTIL (PIPERAZINYL AND/OR HOMOPIPERAZINYL) - ALKANES.

Procedures for the production of new Dibenzo [A, D] cycloheptadienderivaten

Procedure for the production of new Äthanoanthracenderivaten

Procedure for the production of new Äthanoanthracenderivaten as well as their salts

Procedure for the production of new Äthanoanthracenderivaten as well as their salts

As well as procedures for the production of new Amino dihalogenphenyl äthylaminen from their acid addition salts

Procedure for the production of new tricyclischen amines and their acid addition salts

Procedures for the production of Dibenzo [A, D] cycloheptadienderivaten

Procedures for the production of new 1-Amino-4-phenylbicyclo [2,2,2] octanen and of them not toxic salts

Procedure for the production of new Äthanoanthracenderivaten

Procedures for the production of new Dibenzo [A, D] cycloheptatrienderivaten as well as from their acid addition salts and quaternären ammonium derivatives

Phenyl/pyridyl-N-phenyl/pyridyl derivatives for treating RNA virus infection

The present invention relates to a compound of formula (Ic) wherein X ...

Heterocyclic compounds as CCR2b antagonists

CHEMICAL COMPOUNDS FOR THE TREATMENT OF PARKINSONISM.

BENZENESULFONAMIDO-PIPERAZINES AND -PERHIDRO-1,4- DIAZEPINES

PHENYL/PYRIDYL-N-PHENYL/PYRIDYL DERIVATIVES FOR TREATING A RNA VIRUS INFECTION

The present invention relates to a compound of formula (Ie) wherein Y1 represents an aryl group, X2 represents a -O- group, a -NH- group, a -S- group, a-CO-NH- group, a -NH-CO-NH- group, a -NH-CO- group, a -CH(OH)- group, a -CH(COOH)NH- group, a -CH(COOCH3)NH- group, a -C(OH)(CH2OH)-, a (AA) group, a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or heteroatoms, a -SO2- group, or a -SO2-NH- group, Y2 represents a hydrogen atom, a hydroxyl group, a (C1-C4)alkoxy group, a -CHC(OH)2, a COORf, wherein Rf represents a hydrogen atom or a (C1-C4)alkyl group, a morpholinyl group, a dihydropyranyl group, a (BB) group, a (CC) group, a -PO(ORf)(OR'f) group, wherein Rf and R'f independently represents a hydrogen atom or a (C1-C4)alkyl group, an oxetanyl group, a -S?(CH3)3 group, a -NHCOO-(C1-C4)alkyl group, or a -CR1R2R3 group, or any of its pharmaceutically acceptable salt. The present invention further relates to pharmaceutical compositions containing them and to synthesis process for ...

DRUG DERIVATIVES

The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention ...

METHOD FOR PREVENTING AGGLOMERATION OF POWDER

A process for preparing a poly-1,4-ethylenepiperazine, which comprises reacting a piperazine derivative with a dihalogenated alkane.

CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS

Disclosed are compounds of the formulas: wherein Ar is optimally substituted aryl; B is O, S, NR5 or CR5R6; n is 1, 2 or 3; m is 2,3 or 4; W, X, Y and T are each hydrogen or substituent; R1 and R2 are each hydrogen or alkyl; R3 and R4 are each hydrogen, alkyl or alkoxy; R5 is alkyl or aryl; R6 is hydrogen or substituent; and A is hydrogen or substituent. These compounds bind to neuropeptide Y1 (NPY1) reptor and are useful for treating eating disorders such as obesity and bulimia as well as cardiovascular diseases such as hypertension.

1- 2-(2,3-DIHYDRO-1H-INDEN-1-YL)ETHYL -4-(NAPHTH-1-YL) PIPERAZINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

Compounds of general formula (I), wherein X is a hydrogen atom, a hydroxy group, a C1-3 alkoxy group or a cyclopropylmethoxy group, and Y is a hydrogen atom, a hydroxy group or a methoxy group, are provided for therapeutical use.

Verfahren zur Darstellung eines Gemisches bisquaternärer Dimorpholinverbindungen.

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem Ephedrin.

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem Nicotinsäureamid.

Verfahren zur Herstellung von polycyclischen Ammoniumsalzen von Alkylendiaminen

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem Morpholin.

Verfahren zur Herstellung von p-amino-benzolsulfonyl-a-amino-pyridin-Bz-N-methylensulfosaurem Chinin.

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem 4-Dimethylamino-1-phenyl-2,3-dimethylpyrazolon.

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem Piperazin.

Verfahren zur Darstellung eines Calciumsalzes eines Sulfonamids.

Verfahren zur Herstellung von p-amino-benzolsulfonyl- -amino-pyridin-Bz-N-methylensulfosaurem Natrium.

Verfahren zur Darstellung von p-aminobenzolsulfonyl-(a-aminopyridyl)- methylensulfosaurem Hexamethylentetramin.

Verfahren zur Bekämpfung von Insekten.

Verfahren zur Herstellung spasmolytisch wirkender tertiärer Amine

Verfahren zur Herstellung basisch substituierter Malonsäuredinitrile

Procédé de préparation d'un nouveau sel biquaternaire de pentaméthylène-bis-N-(N-méthyl-pyrrolidinium).

Verfahren zur Herstellung von Kunststoffmassen für Schallplatten.

Metodo di alchilazione di ammine cicliche con esteri di acidi carbossilici

Procédé de préparation de diamines

Verfahren zur Herstellung von neuen Sekundär- oder Tertiäraminen mit spasmolytischer Wirkung

Verfahren zur Herstellung analeptisch wirksamer N-substituierter Aminonorcamphanderivate

Procédé de préparation d'un nouveau sel biquaternaire du pentaméthylène-bis-N-(N-méthyl-pyrrolidinium).

Procédé de préparation de sels d'ammonium quaternaires

Verfahren zur Herstellung von Phenyl-cycloalkanmethylaminen

Verfahren zur Herstellung neuer carbocyclischer Verbindungen

Verfahren zur Herstellung von Phenyl-cycloalkanmethylaminen

Verfahren zur Herstellung von neuen Äthanoanthracenderivaten

Verfahren zur Herstellung von neuen Aethanoanthracenderivaten

Verfahren zur Herstellung von Dibenzo-cycloheptenen

Verfahren zur Herstellung von Aminopropyliden-9,10-dihydroanthracenen

Tetrahydro pyrido-or cycloalkyl-pyrazinyl-hydrazines - as antihypertensive agents

Cpds. of formula (I) and their salts: (where R1 is NH2 or -N=C-R3-R4; R3 and R4 are 1-4C alkyl; R2 is 1-4C alkyl or Ph, R8 is H or 1-4C alkyl; A is (CH2)n; and n is 1,2 or 3 and is 2 or 3 when R1 is NH2, R2 is Me or Ph and R8 is H; or A is NCOR5; R5 is 1-6C alkyl, 3-6C alkenyl or (CH2)mR6 and m is 0, 1 or 2 and R6 is phenyl opt. substd. by F, Cl, Br, 1-4C alkyl, -alkoxy or -alkoxy or -alkylthio; or R5 is OR7 and R7 is 1-4C alkyl, 2-4C alkenyl, 7-10c phenylalkyl or 8-10C phenylalkenyl opt. substd. in the ring by Cl, 1-4C alkyl or alkoxy) are antihypertensive agents.

Verfahren zur Herstellung von Derivaten von Guanidin

Verfahren zur Herstellung von neuen Amino-dihalogen-phenyläthylaminen

Verfahren zur Herstellung von neuen Amino-dihalogenphenyläthylaminen

Procédé de préparation de pipérazinodibenzocycloheptadiènes

Procédé de préparation de nouvelles amines substituées sur l'azote

Verfahren zur Herstellung photographischer Bilder

Verfahren zur Herstellung von Isothiouronium-Verbindungen

Verfahren zur Herstellung von organischen Aminen

Procédé de préparation de nouveaux dérivés du dibenzo (a,d) cycloheptadiène

Procédé de préparation de nouveaux dérivés du dibenzo (a,d) cycloheptadiène

Verfahren zur Herstellung von Enaminen

Procédé de préparation d'un sel de pyrazolidine substituée

Guanidines and isothioureas adjuvants for diptheria and

... (A) Cpds. contng. a cation (CH3(CH2)m-A-(CH2)n-XC(NHR2)NHR')+ (I) and corresp. free bases. Where R' = (1-4C) alkyl R2 = (1-4C) alkyl or 2-phenoxyethyl X = NH or S A = O or methylene n = 2-3 m = 11-15. (B) Antigenic vaccines contg. (I) particularly tetanus toxoid. Adjuvants for diphtheria and tetanus vaccines to improve their antigenic properties. Salts of N-2-dodecyloxyethyl-(II), N-3-dodecyloxypropyl-, N-2-hexadecyloxyethyl-, N'N"-dimethylguanidinium cation and of N-hexadecyl-N'-methyl-N"-2-phenoxyethylguanidium cation. Salts of S.hexadecyl and S.octadecyl-N, N'-dimethylthiuronium and their use in prepn. of (I).

Alkoxymethylamine useful as stabilisers processing aids

Alkoxymethylamines are produced by reacting hemiformals with primary or secondary amines, opt. in presence of solvent. Yields are high and only equiv. amts. of reactants are needed. Temp. can be controlled easily by adjusting rate at which components are mixed. As intermediates, stabilisers, processing aids and curing agents for plastics.

PROCEDE DE PREPARATION DE TETROLS.

PROCEDE DE PREPARATION DE DERIVES D'INDANTETROL.

PROCEDE DE PREPARATION DE TETROLS.

Synthetic aromatising and perfuming cpds - contg. substd. isopropyl-diones/ketones /alcohols, for esp., foods, tobaccos and pharmaceuticals

Aroma of foodstuffs for human and animal nutrition, beverages, partic. teas, pharmaceuticals, tobacco or tobacco substitute, perfume compsns. and perfumed product can be improved, reinforced or modified with 1-500 (10-50) ppm of (a) 6-Me-3-isopropyl-hepta-4,6-dien-1-ol; (b) 8-OH-5-isopropyl-non-6-en-2-one; (c) 5-isopropyl-non-3-ene-2,8-diol; (d) 8-OH-5-isopropyl-nonan-2-one, (e) 5-isopropyl-nonane-2,8-diol; (f) 5-isopropyl-nonane-2,8-dione; (g)3,4-epoxy-5-isopropyl-nonane-2,8-dione; (h) 8-OH-5-isopropyl-8-Me-non-6-en-2-one; (i) 6,7-epoxy-8-OH-5-isopropyl-8-Me-nonan-2-one. (j) 2-isopropyl-5-Me-6,8-dioxa-bicyclo 3,2,1 -octan-7-yl-methyl-keton- e; (k) 2-(2-isopropyl-5-Me-6,8-dioxa-bicyclo 3,2,1 -octan-7-yl)-propan-2- -ol, (1) 6-isopropyl-1,3,5-trimethyl-2,9-dioxabicyclo- 3,3,1 -nonan-4-ol and (m) 1-(2-isopropyl-5-Me-6,8-dioxa-bicyclo 3,2,1 -octan-7-yl)-ethan-1-ol.

Verfahren zur Herstellung basischer Fluoren-Derivate

Procédé de préparation d'amines dérivées du dibenzo (a,d) (1,4) cycloheptadiène

Verfahren zur Herstellung von 9,10-Dihydroanthracenen

Verfahren zur Herstellung neuer Cyclohexanderivate

Procédé de préparation de nouveaux dérivés de la quinoléine

Verfahren zur Herstellung eines neuen Sekundär- oder Tertiäramins mit spasmolytischer Wirkung

Verfahren zur Herstellung von Phenyl-cycloalkanmethylaminen

Verfahren zur Herstellung von Phenyl-cycloalkanmethylaminen

Verfahren zur Herstellung von 3-Azabicyclo-(3,2,2)-nonan-Derivaten

Procédé de préparation de nouveaux dérivés du dibenzocycloheptatriène

Verfahren zur Herstellung polyquaternärer Verbindungen und deren Anwendung

Verfahren zur Herstellung von quarternären Ammoniumverbindungen

Verfahren zur Herstellung neuer wasserlöslicher Aminomethylverbindungen der Tetracyclinreihe

Verfahren zur Herstellung von a,a-Diphenyl- -hexamethylenimino-butyramid

Procédé de préparation de composés hétérocycliques contenant de l'azote nucléaire

Salt forms of [R-(R*,R*)]-2-(4-flurorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Method for producing alcohol and/or amine from amide compound

Disclosed herein is a method for producing an alcohol and an amine from an amide under an atmosphere of hydrogen with the use of, as a catalyst, a ruthenium complex that is easily prepared, easy to handle, and relatively cheaply obtained. Specifically, the method is a method for producing an alcohol and/or an amine from an amide compound under an atmosphere of hydrogen with the use of as a catalyst, a ruthenium carbonyl complex represented by the following general formula (1): RuXY(CO)(L) (1) wherein X and Y may be the same or different from each other and each represents an anionic ligand and L represents a tridentate aminodiphosphine ligand containing two phosphino groups and a —NH— group.

TRANSAMINATION OF NITROGEN-CONTAINING COMPOUNDS TO MAKE CYCLIC AND CYCLIC/ACYCLIC POLYAMINE MIXTURES

A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses. 1. A method of making a cyclic polyamine-containing product mixture comprising the steps of:(a) providing a reaction composition comprising one or more nitrogen-containing compounds having a binary component that has at least two non-tertiary amine groups separated from one another by a binary carbon atom spacing (C2 spacing) and, optionally, a second component that has at least two nitrogen containing groups separated from one another by a second carbon atom spacing; and(b) subjecting the reaction composition to a transamination reaction in the presence of a hydrogenation/dehydrogenation catalyst to obtain the cyclic polyamine-containing mixture.2. A method of making a cyclic polyamine-containing product mixture , comprising the steps of:(a) providing information indicative of a transamination product mixture composition as a function of a molar ratio of a reaction composition having a binary component that has at least two non-tertiary amine groups separated from one another by a binary carbon atom spacing (C2 spacing) and, a second component that has at least two nitrogen containing groups separated from one another by a second carbon atom spacing; and(b) using the information to provide the reaction mixture; and(c) subjecting the reaction mixture to a transamination reaction in the presence of a hydrogenation/dehydrogenation catalyst.3. The method of claim 1 , wherein the binary and second components are provided in a single nitrogen-containing compound.4. A method of making ...

Novel ruthenium complexes and their uses in processes for formation and/or hydrogenation of esters, amides and derivatives thereof

The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.

PALLADIUM CATALYST, METHOD FOR ITS PREPARATION AND ITS USE

The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. 2. The composition of in a solid form.3. The composition of having a melting point of 220° C. as determined by DSC in inert atmosphere.4. The composition of claim 1 , having a decomposition point of 169.5° C. as determined by DSC in air under atmospheric pressure.5. A palladium(0) complex comprising three fluorinated phosphine compounds.6. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 4 months of storage in air at a temperature of 25° C.7. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 20 months of storage in air at room temperature.8. The palladium(0) complex of having a melting point in inert atmosphere of 220° C.9. The palladium(0) complex of exhibiting stability at any temperature below its melting point.10. The palladium(0) complex of exhibiting insolubility in water at industrially relevant temperatures and stability when stored in water.11. The palladium(0) complex of comprising a yellow solid.12. The palladium(0) complex of that dissolves at around 90° C. in aqueous alcohols.13. The palladium(0) complex of having catalytic activity in cross coupling reactions at a concentration of from 0.1 to 0.3 mole % of the substrate.14. A method for catalysing a C—C claim 5 , C-heteroatom claim 5 , or hydrogenation reaction comprising carrying out the C—C claim 5 , C-heteroatom or hydrogenation reaction in the presence of the palladium(0) complex of .15. The method of claim 14 , wherein the reaction is a C—C cross-coupling reaction.16. The method of claim 14 , wherein the C—C cross-coupling reaction is selected from the group consisting of: Suzuki coupling claim 14 , Heck coupling and ...

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

Processes for preparing amines and catalysts for use therein

Processes for preparing an amine are described which comprise reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia, primary and secondary amines, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst. The catalytically active composition of the catalyst, before its reduction with hydrogen, comprises oxygen compounds of zirconium, of copper, of nickel, in the range from 1.0 to 5.0% by weight of oxygen compounds of cobalt, calculated as CoO, and in the range from 0.2 to 5.0% by weight of oxygen compounds of sulfur, of phosphorus, of gallium, of lead and/or of antimony, calculated in each case as H2SO4, H3PO4, Ga203, PbO and Sb203 respectively.

Process for Preparing Piperazine

Process for preparing piperazine of the formula I 132-. (canceled)34. The process according to claim 33 , wherein the catalytically active mass of the catalyst claim 33 , prior to its reduction with hydrogen claim 33 , comprises 20 to 65% by weight of oxygen-containing compounds of zirconium claim 33 , calculated as ZrO.35. The process according to claim 33 , wherein the catalytically active mass of the catalyst claim 33 , prior to its reduction with hydrogen claim 33 , comprises 2 to 25% by weight of oxygen-containing compounds of copper claim 33 , calculated as CuO.36. The process according to claim 33 , wherein the catalytically active mass of the catalyst claim 33 , prior to its reduction with hydrogen claim 33 , comprises 15 to 50% by weight of oxygen-containing compounds of nickel claim 33 , calculated as NiO.37. The process according to claim 33 , wherein the catalytically active mass of the catalyst claim 33 , prior to its reduction with hydrogen claim 33 , comprises 0.1 to 3% by weight of oxygen-containing compounds of molybdenum claim 33 , calculated as MoO.38. The process according to claim 33 , wherein the molar ratio of nickel to copper is greater than 1.39. The process according to claim 33 , wherein no rhenium and/or ruthenium is present in the catalytically active mass of the catalyst.40. The process according to claim 33 , wherein no iron and/or zinc is present in the catalytically active mass of the catalyst.41. The process according to claim 33 , wherein no cobalt is present in the catalytically active mass of the catalyst.42. The process according to claim 33 , wherein no oxygen-containing compounds of silicon and/or of aluminum and/or of titanium are present in the catalytically active mass of the catalyst.43. The process according to claim 33 , wherein the reaction is carried out at a temperature in the range from 185 to 215° C.44. The process according to claim 33 , wherein the reaction is carried out at an absolute pressure in the range from ...

Phenyl amino pyrimidine compounds and uses thereof

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Diamine and meglumine salt forms of fatty acids

Provided herein are diamine salts of eicosapentaenoic acid and docosahexaenoic acid, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and the uses of such compounds as agents for treating dyslipidemia, cardiovascular diseases such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke and obesity.

New palladium catalyst, method for its preparation and its use

The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

Process for Preparing Pyrrolidine

Process for preparing pyrrolidine of the formula I 128-. (canceled)30. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from 0.4 to 4.0% by weight of oxygen-containing compounds of tin claim 29 , calculated as SnO.31. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from 0.6 to 3.0% by weight of oxygen-containing compounds of tin claim 29 , calculated as SnO.32. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from 5.0 to 35% by weight of oxygen-containing compounds of cobalt claim 29 , calculated as CoO.33. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from 10 to 30% by weight of oxygen-containing compounds of cobalt claim 29 , calculated as CoO.34. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from{'sub': 2', '3, '15 to 80% by weight of oxygen-containing compounds of aluminum, calculated as AlO,'}1.0 to 20% by weight of oxygen-containing compounds of copper, calculated as CuO, and5.0 to 35% by weight of oxygen-containing compounds of nickel, calculated as NiO.35. The process according to claim 29 , wherein the catalytically active mass of the catalyst claim 29 , prior to its reduction with hydrogen claim 29 , comprises in the range from{'sub': 2', '3, '30 to 70% by weight of oxygen-containing compounds of aluminum, calculated as AlO,'}2.0 to 18% by weight of oxygen-containing compounds of copper, calculated as CuO, and10 to 30% by weight of oxygen- ...

PROCESS FOR PREPARING AMINES BY HOMOGENEOUSLY CATALYZED ALCOHOL AMINATION IN THE PRESENCE OF A COMPLEX CATALYST COMPRISING IRIDIUM AND AN AMINO ACID

The invention relates to a process for preparing amines (A) by alcohol amination of alcohols (Al) by means of an aminating agent (Am) with elimination of water, wherein the alcohol amination is carried out in the presence of a complex catalyst comprising iridium and an amino acid. 1. A process for preparing an amine by amination of an alcohol , the process comprising aminating an alcohol with an aminating agent in the presence of a complex catalyst comprising iridium and an amino acid , to form an amine and with elimination of water.2. The process according to claim 1 , wherein the complex catalyst comprises an α-amino acid.3. The process according to claim 1 , wherein the process is homogeneously catalyzed.5. The process according to claim 4 , wherein:{'sup': 3', '4', '5', '6', '7, 'R, R, R, Rand Reach represent methyl; and'}X represents chloride.6. The process according to claim 1 , wherein the amino acid is selected from the group consisting of alanine claim 1 , valine claim 1 , leucine claim 1 , isoleucine claim 1 , proline claim 1 , tryptophan claim 1 , phenylalanine claim 1 , methonine claim 1 , glycine claim 1 , serine claim 1 , tyrosine claim 1 , threonine claim 1 , cysteine claim 1 , asparagine claim 1 , glutamine claim 1 , aspartate claim 1 , glutamate claim 1 , lysine claim 1 , arginine claim 1 , histidine claim 1 , citrulline claim 1 , homocysteine claim 1 , homoserine claim 1 , (4R)-4-hydroxyproline claim 1 , (5R)-5-hydroxylysine claim 1 , ornithine and sarcosine.7. The process according to claim 1 , wherein the process occurs at temperatures in the range from 50° C. to 150° C.8. The process according to claim 1 , wherein the process occurs without the addition of a base selected from the group consisting of an alkali metal hydroxides claim 1 , an alkaline earth metal hydroxide claim 1 , an alkali metal alkoxide claim 1 , an alkaline earth metal alkoxide claim 1 , an alkali metal carbonate claim 1 , an alkaline earth metal carbonate claim 1 , an alkali ...

Immobilized Ruthenium-Triphos Catalysts for Selective Hydrogenolysis of Amides

A compound represented by the structure of formula (I): 5. The compound of claim 4 , wherein L comprises trimethylenemethane.7. The method of claim 6 , wherein the Ru-containing compound comprises [Ru(COD)(methylallyl)].8. A catalyst composition comprising:(a) an oxidic support; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, '(b) the compound of immobilized on the support.'}9. The catalyst composition of claim 8 , wherein the oxidic support comprises silica claim 8 , magnesia claim 8 , titania claim 8 , or alumina.10. The catalyst composition of claim 8 , wherein the oxidic support comprises silica.11. The catalyst composition of claim 8 , wherein L comprises trimethylenemethane.13. The process of claim 12 , wherein the oxidic support comprises silica claim 12 , magnesia claim 12 , titania claim 12 , and alumina.14. The process of claim 12 , wherein the oxidic support comprises silica.15. The process of claim 12 , wherein L comprises trimethylenemethane.16. The process of claim 13 , wherein L comprises trimethylenemethane.17. The process of claim 14 , wherein L comprises trimethylenemethane.18. The process of claim 12 , wherein the amide comprises a lactam.19. The process of claim 13 , wherein the amide comprises a lactam.20. The process of claim 17 , wherein the amide comprises a lactam. This is application claims the benefit of Provisional Application No. 62/691,936 filed on Jun. 29, 2018 under 35 U.S.C. § 119(e)(1); the entire content of the provisional application is hereby incorporated by reference.The invention generally relates to the field of organic chemistry. It particularly relates to silyl ether triphos compounds, organometallic complexes containing the silyl ether triphos compounds, catalysts containing the organometallic complexes immobilized on oxidic supports, methods of making, and/or methods of using the compounds, complexes, and catalysts.The hydrogenolysis of amides to amines under mild reaction conditions represents a challenging chemical ...

Calpain modulators and therapeutic uses thereof

Small molecule calpain modulator compounds, including their pharmaceutically acceptable salts, can be included in pharmaceutical compositions. The compounds can be useful in inhibiting calpain, or competitive binding with calpastatin, by contacting them with CAPN1, CAPN2, and/or CAPN9 enzymes residing inside a subject. The compounds and composition can also be administered to a subject in order to treat a fibrotic disease or a secondary disease state or condition of a fibrotic disease.

Amine salts of prostaglandin analogs

The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.

PROCESS FOR REMOVING METHOXYETHANOL FROM A MIXTURE COMPRISING METHOXYETHANOL AND MORPHOLINE

A method for removing methoxyethanol from a mixture comprising methoxyethanol and morpholine makes use of the selective adsorption of methoxyethanol onto a mixed oxide comprising a spinel phase. The mixed oxide comprises 20 to 30% by weight MgO and 80 to 70% by weight AlO. The spinel phase has the formula MgAlO. The mixture is a pre-purified reaction output of the reaction of diethylene glycol with ammonia in the presence of an amination catalyst. 1. A method for removing methoxyethanol from a mixture comprising methoxyethanol and morpholine by selective adsorption of methoxyethanol onto a mixed oxide comprising a spinel phase.2. The method according to claim 1 , wherein the spinel phase has the formula{'br': None, 'sub': 2', '4, 'ABO'}in whichA is a divalent cation; andB is a trivalent or tetravalent cation.3. The method according to claim 2 , wherein the spinel phase has the formula MgAlO.4. The method according to claim 3 , wherein the mixed oxide comprises 20 to 30% by weight MgO and 80 to 70% by weight AlO.5. The method according to claim 1 , wherein the mixture is passed over a bed of the mixed oxide.6. The method according to claim 1 , wherein the mixture comprises in addition at least one component selected from 1 claim 1 ,2-ethylenediamine claim 1 , methoxyethylmorpholine and formylmorpholine.7. The method according to claim 1 , wherein the mixture is dried prior to the selective adsorption.8. The method according to claim 7 , wherein the mixture is dried by bringing it into contact with a molecular sieve.9. The method according to claim 1 , wherein the mixed oxide is regenerated by treatment with water.10. The method according to claim 9 , wherein coadsorbed morpholine is desorbed prior to the regeneration of the mixed oxide.11. The method according to claim 10 , wherein coadsorbed morpholine is desorbed by passing over an inert gas or an inert gas containing steam.12. The method according to claim 11 , wherein the desorbed coadsorbed morpholine is ...

Hydrogenation reaction catalyst used to hydrogenate amide compound and method for producing amine compound using same

A catalyst, which can be used even under mild conditions and also has durability so as to enable repeated use while maintaining high activity, and with which a reduction reaction for converting an amide compound into an amine compound can be carried out, is provided by means of an amide compound hydrogenation reaction catalyst characterized in that platinum and vanadium are supported on a carrier and a method for producing an amine compound using the same.

JOINT PRODUCTION METHOD AND DEVICE FOR AZIRIDINE, PIPERAZINE AND TRIETHYLENEDIAMINE

Disclosed are a joint production method and device for aziridine, piperazine and triethylenediamine. The method comprises: reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material under the existence of a cyclamine catalyst; reaction 2, preparing aziridine by taking the ethanol amine as the raw material under the existence of a catalyst B; and taking heat released in the reaction 1 as a heat source of heat absorption in the reaction 2. The device comprises a reactor 1 for carrying out the reaction 1 and the heat exchange between reaction materials of the reaction 1 and the raw material of the reaction 2 and a reactor 2 for carrying out the reaction 2. According to the present invention, the same raw material, namely the ethanol amine is adopted, aziridine, piperazine and triethylenediamine can be produced in a joint manner, the heat released in the reaction 1 is used for preheating materials in the reaction 2, so that heat coupling between the reactions is implemented, energy conservation is facilitated and competitiveness of the device is improved. 1. A joint production method for aziridine , piperazine and triethylenediamine , characterized in that , the method comprises:reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material in the presence of a cyclamine catalyst; andreaction 2, preparing aziridine by taking the ethanol amine as a raw material in the presence of a catalyst B;{'sub': a', 'b', 'c', 'd', 'e', 'f, 'wherein the catalyst B is TiPBXYO, wherein: X is an alkaline earth metal, Y is an alkaline metal, 0 is an oxygen element; a, b, c, d, e, and f are the mole ratios of each element atom, and a=1, b=0.02˜0.2, c=0.002˜0.02, d=0.01˜0.1, e=0.001˜0.01, and f is dependent on a, b, c, d, and e;'}the heat released in the reaction 1 is used as a heat source for the reaction 2.2. The joint production method for aziridine claim 1 , piperazine and triethylenediamine of claim 1 , ...

Organo-1-oxa-4-azonium cyclohexane compounds

Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.

PROCESS TO PREPARE HIGHER ETHYLENE AMINES AND ETHYLENE AMINE DERIVATIVES

The present invention relates to a process to prepare ethyleneamines of the formula NH—(CH—NH—)H wherein p is at least 2 wherein one or more units —NH—CH—NH— are present as a piperazine unit or precursors thereof wherein optionally one or more units —NH—CH—NH— are present as a cyclic ethylene urea unit or between two units —NH—CH—NH— a carbonyl moiety is present, by reacting an ethanolamine-functional compound, an amine-functional compound in the presence of a carbon oxide delivering agent, wherein at least one of the amine-functional compound or the ethanolamine-functional compound contains a piperazine unit, and the reaction is performed in a liquid that comprises water. 2. Process of claim 1 , wherein the ethanolamine-functional compound is of the formula HO—(CH—NH—)H wherein q is at least 1 and the amine functional compound is of the formula NH—(CH—NH—)H wherein r is at least 1 claim 1 , wherein at least one q or r unit is present as a piperazine unit claim 1 , and wherein optionally one or more q or r units may be present as a cyclic ethylene urea claim 1 , cyclic ethylene carbamate or a further piperazine unit.3. Process of wherein the amine-functional compound is piperazine (PIP) claim 1 , aminoethylpiperazine (AEP) claim 1 , or diaminoethylpiperazine (DAEP) claim 1 , piperazinoethyl ethylenediamine (PEEDA) claim 1 , or a linear urea derivative thereof.4. Process of wherein the ethanolamine-functional compound is monoethanolamine (MEA) or aminoethylethanolamine (AEEA) or a cyclic or linear carbamate or urea derivative thereof.5. Process of wherein the liquid comprises at least 75 wt-% of water on total liquid weight.6. Process of wherein the molar ratio of water to the amine-functional compound is greater than 0.2:1 claim 1 , preferably greater than 0.5:1 and most preferably greater than 1:1.7. Process of wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is at least 0.7:1.8. Process of wherein the molar ratio of carbon ...

SALTS OF BICYCLO-SUBSTITUTED PYRAZOLON AZO DERIVATIVES, PREPARATION METHOD AND USE THEREOF

The pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description. 1. (canceled)3. The method according to claim 2 , wherein the pharmaceutical salt is co-administered with a drug selected from the group consisting of a colony stimulating factor claim 2 , a cytokine claim 2 , a chemokine claim 2 , an interleukin or cytokine receptor agonist or antagonist claim 2 , a soluble receptor claim 2 , a receptor agonist or antagonist antibody claim 2 , or one or more peptides or small molecule compounds that have the same mechanism as the drug.4. The method according to claim 2 , wherein the pharmaceutical salt is in the form of an oral dosage form.5. The method according to claim 2 , wherein the dosage form is a parenteral dosage form.6. The method of claim 2 , wherein the pharmaceutically acceptable salt of the compound having formula (I) is a base addition salt.7. The method of claim 2 , wherein the pharmaceutically acceptable salt of the compound having formula (I) is selected from the group consisting of sodium salt claim 2 , lithium salt claim 2 , potassium salt claim 2 , calcium salt claim 2 , magnesium salt claim 2 , arginine salt claim 2 , lysine salt claim 2 , methanamine salt claim 2 , dimethylamine salt claim 2 , trimethylamine salt claim 2 , ethylamine salt claim 2 , diethylamine salt claim 2 , triethylamine salt claim 2 , ethanolamine salt claim 2 , piperazine salt claim 2 , dibenzyl ethylenediamin salt claim 2 , meglumine salt claim 2 , tromethamine salt claim 2 , tetramethyl quaternary ammonium salt claim 2 , tetraethyl quaternary ammonium salt claim 2 , choline salt claim 2 , and combinations thereof.8 ...

PROCESS FOR PRODUCING AN AMINOPROPYNE OR ENAMINONE

There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol. 1. A process for producing an aminopropyne comprising the step of reacting a metal acetylide , an amine and a carbonyl-containing compound in the presence of a transition metal catalyst.2. The process as claimed in claim 1 , wherein said aminopropyne has a terminal alkyne group.3. The process as claimed in claim 1 , wherein said metal acetylide has the structure MC claim 1 , where M is a metal selected from the group consisting of an alkali metal claim 1 , an alkaline earth metal and a transition metal; or wherein said metal acetylide is selected from the group consisting of calcium carbide (CaC) claim 1 , lithium acetylide (LiC) and lanthanium acetylide (LaC).4. (canceled)5. The process as claimed in claim 1 , wherein the transition metal of said transition metal catalyst is selected from the group consisting of copper claim 1 , silver and gold; wherein the copper catalyst is selected from the group consisting of copper chloride claim 1 , copper bromide claim 1 , copper iodide claim 1 , copper fluoride claim 1 , copper acetate and copper acetylacetonate.6. (canceled)7. The process as claimed in claim 1 , wherein said carbonyl-containing compound is an aldehyde having the structure RCHO claim 1 , where Ris selected from aryl or C-alkyl claim 1 , said aryl being optionally substituted by at least one of halide claim 1 , nitrile claim 1 , C-alkyl claim 1 , C-alkoxide ...

SYNERGISTIC COMPOSITIONS

The present invention describes a synergistic composition comprising of one or more statins, or one or more dipeptidyl peptidase IV (DPP IV) inhibitor or one or more biguanide antihyperglycaemic agent and a PPAR agonist of formula (Ia) 2. The synergistic composition as claimed in claim 1 , wherein the one or more DPP IV inhibitors are selected from Sitagliptin claim 1 , Vildagliptin claim 1 , Saxagliptin claim 1 , Alogliptin and Linagliptin.3. The synergistic composition as claimed in claim 1 , wherein the one or more statins are selected from Lovastatin claim 1 , Pravastatin claim 1 , Fluvastatin claim 1 , Simvastatin claim 1 , Atorvastatin claim 1 , Rosuvastatin and Pitavastatin.4. The synergistic composition as claimed in claim 1 , wherein the one or more biguanide antihyperglycaemic agents are selected from Metformin claim 1 , Buformin or Phenformin.5. The synergistic composition as claimed in claim 1 , wherein the one or more thiazolidinediones are selected from Pioglitazone and Rosiglitazone.6. The synergistic composition as claimed in claim 1 , wherein the one or more sulphonylureas are selected from glibenclamide claim 1 , glipizide claim 1 , gliclazide claim 1 , glimepiride claim 1 , tolazamide claim 1 , tolbutamide claim 1 , acetohexamide claim 1 , carbutamide claim 1 , chlorpropamide claim 1 , glibomuride claim 1 , gliquidone claim 1 , glisentide claim 1 , glisolamide claim 1 , glisoxepide claim 1 , glyclopyamide claim 1 , glycylamide and glipentide.7. The synergistic composition as claimed in claim 1 , wherein the one or more SGLT-2 inhibitors are selected from Dapagliflozin claim 1 , Canagliflozin claim 1 , Empagliflozin claim 1 , Ertugliflozin and Ipragliflozin.8. The synergistic composition as claimed in claim 1 , wherein the one or more GLP-1 agonists are selected from Exenatide claim 1 , Liraglutide and Dulaglutide.9. (canceled)10. A method for the treatment of dyslipidemia claim 1 , hypertriglyceridemia or diabetes mellitus which comprises ...

SELECTIVE HYDROGENATION CATALYST AND SELECTIVE HYDROGENATION METHOD USING THE SAME

The present invention relates to a Ru—Pd bimetallic catalyst for use in hydrogenation of a compound, and more particularly to a catalyst prepared by loading both ruthenium and palladium on a g-CNsupport and to a selective hydrogenation process of a pyridine group in a reaction system containing both a pyridine group and a benzene group using the catalyst. 2. The selective hydrogenation catalyst of claim 1 , wherein a weight ratio (b/a) of the ruthenium (b) relative to the palladium (a) ranges from 0.25 to 10.3. A method of preparing a selective hydrogenation catalyst claim 1 , comprising:{'sub': 3', '4, 'a) preparing a support solution by dispersing a g-CNsupport in distilled water;'}b) preparing a catalyst precursor solution by adding the support solution with a ruthenium precursor and a palladium precursor such that a sum of weights of ruthenium and palladium as active components is 0.1 to 15 wt % based on a total weight of the catalyst including the support; andc) drying the catalyst precursor solution and then performing heat treatment in a hydrogen atmosphere.4. The method of claim 3 , wherein claim 3 , in step b) claim 3 , a weight ratio (b/a) of the ruthenium (b) relative to the palladium (a) ranges from 0.25 to 10.5. The method of claim 3 , wherein claim 3 , in step c) claim 3 , the heat treatment in the hydrogen atmosphere is performed at a temperature ranging from 250 to 500° C.7. The selective hydrogenation method of claim 6 , wherein the benzene compound is at least one selected from among benzene claim 6 , toluene claim 6 , xylene claim 6 , cyclohexyltoluene claim 6 , diphenylmethane claim 6 , benzyl alcohol claim 6 , phenylethyl alcohol claim 6 , methyl phenyl ether claim 6 , and ethyl phenyl ether.8. The selective hydrogenation method of claim 6 , wherein the pyridine compound is at least one selected from among pyridine claim 6 , methylpyridine claim 6 , ethylpyridine claim 6 , cyclohexyl methylpyridine claim 6 , benzylpyridine claim 6 , ...

RHENIUM RECOVERY FROM USED REDUCTIVE AMINATION CATALYSTS

The present invention provides techniques that selectively recover Re from reductive amination catalysts. In particular, the present invention allows Re to be recovered selectively relative to Ni, Co, and/or Cu, and particularly Ni, that are often present on reductive amination catalysts. The present invention uses a combination of oxidation and extraction techniques to selectively recover Re relative to Ni, Co, and/or Cu. Advantageously, the recovery is selective even when using aqueous solutions for extraction. 1. A method for recovering rhenium from a reductive amination catalyst , comprising the steps of:a) providing a heterogeneous catalyst that has been used in a reducing atmosphere to carry out a reductive amination, wherein the catalyst comprises a substrate and at least one species comprising rhenium and at least one species comprising nickel supported on the substrate, wherein the at least one species comprising rhenium has a first solubility in a liquid carrier, and wherein the substrate comprises at least 15 weight percent alumina based on the total weight of the substrate;b) causing the catalyst to contact the liquid carrier in the presence of heat and at least one oxidizing agent under conditions effective to convert at least a portion of the Re-containing species into a Re-containing product that has a second solubility in the liquid carrier, wherein the second solubility is greater than the first solubility; andc) extracting the Re-containing product into the liquid carrier.2. The method of claim 1 , wherein the substrate comprises a guest/host structure and the heterogenous catalyst is supported at least upon the guest particles.3. The method of claim 1 , wherein step (a) comprises calcining and reducing the substrate.4. The method of claim 1 , wherein the substrate comprises alumina and silica.5. The method of claim 1 , wherein the heterogeneous catalyst further comprises at least one of a Co-containing species and a Cu-containing species.6. The ...

Catalysts and processes for the hydrogenation of amides

There is provided a process for the reduction of one or more amide moieties in a compound comprising contacting the compound with hydrogen gas and a transition metal catalyst in the presence or absence of a base under conditions for the reduction an amide bond. The presently described processes can be performed at low catalyst loading using relatively mild temperature and pressures, and optionally, in the presence or absence of a base or high catalyst loadings using low temperatures and pressures and high loadings of base to effect dynamic kinetic resolution of achiral amides.

JOINT PRODUCTION METHOD AND DEVICE FOR AZIRIDINE, PIPERAZINE AND TRIETHYLENEDIAMINE

Disclosed are a joint production method and device for aziridine, piperazine and triethylenediamine. The method comprises: reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material under the existence of a cyclamine catalyst; reaction 2, preparing aziridine by taking the ethanol amine as the raw material under the existence of a catalyst B; and taking heat released in the reaction 1 as a heat source of heat absorption in the reaction 2. The device comprises a reactor for carrying out the reaction 1 and the heat exchange between reaction materials of the reaction 1 and the raw material of the reaction 2 and a reactor for carrying out the reaction 2. According to the present invention, the same raw material, namely the ethanol amine is adopted, aziridine, piperazine and triethylenediamine can be produced in a joint manner, the heat released in the reaction 1 is used for preheating materials in the reaction 2, so that heat coupling between the reactions is implemented, energy conservation is facilitated and competitiveness of the device is improved. 15-. (canceled)6. A device for production of aziridine , piperazine and triethylenediamine , the device comprising:a first reactor, for carrying out a first reaction and for heat exchange between reaction materials of the first reaction and raw materials of a second reaction;a second reactor, for carrying out the second reaction; anda combination separation unit, comprising a flash unit, an aziridine separation unit, and a polyamine separation unit connected successively, wherein the flash unit is configured for separating nitrogen, the aziridine separation unit is configured for separating aziridine, and the polyamine separation unit is configured for separating piperazine and triethylenediamine.7. The device of claim 6 , wherein the flash unit is a flash tower having a theoretical plate number of 1 to 3 claim 6 , and is configured for operation at a temperature in a range of 0° C. ...

HYDROGENATION CATALYST USED IN AMIDE COMPOUND HYDROGENATION AND METHOD FOR PRODUCING AMINE COMPOUND USING SAME

Provided is a catalyst for amide compound hydrogenation characterized in that rhodium and molybdenum are supported on hydroxyapatite, the catalyst for amide compound hydrogenation providing a catalyst that can promote a reduction reaction that converts an amide compound into an amine compound, can be used under moderate conditions, and has durability that allows repeated use thereof while retaining high activity. Also provided is a method for producing an amine compound, the method being characterized by including bringing an amide compound into contact with the catalyst for amide compound hydrogenation to cause hydrogenation, thereby producing an amine compound. 1. A catalyst for amide compound hydrogenation , the catalyst comprisinghydroxyapatite, andrhodium and molybdenum that are supported on the hydroxyapatite.2. The catalyst for amide compound hydrogenation according to claim 1 , wherein the amide compound is a secondary or higher amide compound or an amide compound having an aromatic substituent.3. A method for producing an amine compound claim 1 , the method comprising bringing an amide compound into contact with the catalyst for amide compound hydrogenation according to to cause hydrogenation of the amide compound claim 1 , thus producing an amine compound.4. The method for producing an amine compound according to claim 3 , wherein the hydrogenation is performed at 100° C. or lower.5. The method for producing an amine compound according to claim 3 , wherein the hydrogenation is performed at 5 MPa or less.6. The method for producing an amine compound according to claim 3 , wherein the amide compound is brought into contact also with molecular sieve.7. The method for producing an amine compound according to claim 3 , wherein the amide compound is a secondary or higher amide compound or an amide compound having an aromatic substituent.8. A method for producing the catalyst for amide compound hydrogenation according to claim 1 , the method comprising allowing ...

NOVEL RUTHENIUM COMPLEXES AND THEIR USES IN PROCESSES FOR FORMATION AND/OR HYDROGENATION OF ESTERS, AMIDES AND DERIVATIVES THEREOF

The present invention relates to novel Ruthenium complexes and related borohydride complexes, and their use for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including preparing polyamides (e.g., polypeptides) by reacting dialcohols and diamines or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones), cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to novel uses of certain pyridine Ruthenium complexes. 4. The process according to claim 1 , wherein Xand/or Xare absent claim 1 , and the pyridyl or bipyridy moiety is unsubstituted.5. The process according to claim 1 , wherein Lis phosphine (PRR).13. The process according to claim 10 , wherein Xand/or Xare absent claim 10 , and the pyridyl or bipyridy moiety is unsubstituted.14. The process according to claim 10 , wherein Lis phosphine (PRR).16. The process of claim 10 , for preparing an amide from amine and an alcohol claim 10 , wherein the process is for preparing a polypeptide or a cyclic dipeptide claim 10 , and wherein the primary or secondary amine and the primary alcohol are a beta-aminoalcohol. This application is a Divisional Application from U.S. application Ser. No. 14/702,641 filed May 1, 2015, which is a Divisional Application from U.S. application Ser. No. 13/880,328 filed Jun. 11, 2013 now U.S. Pat. No. 9,045,381, ...

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MULTIPLE SCLEROSIS

The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of salts of formula I or formula II; and methods for treating or preventing multiple sclerosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of neurodegenerative diseases and psoriasis. 3. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.4. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 3 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 3 , delayed release or sustained release claim 3 , transmucosal claim 3 , syrup claim 3 , topical claim 3 , parenteral administration claim 3 , injection claim 3 , subdermal claim 3 , oral solution claim 3 , rectal administration claim 3 , buccal administration or transdermal administration.6. The pharmaceutical composition of claim 4 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration or transdermal administration.7. Compounds and compositions of are formulated for the treatment of neurodegenerative diseases claim 5 , multiple sclerosis claim 5 , psoriasis and inflammatory diseases.8. Compounds and compositions of are formulated for the treatment of neurodegenerative diseases claim 6 , ...

Use of type of compounds as energy-containing material

The present application belongs to the field of energetic compounds, and particularly relates to the use of a perovskite-type compound ABX3 as an energetic material. As a finding of the present application, the structural characteristics of the perovskite type enables the type of compound to be highly stable, thus overcoming the unsafety of an explosive having poor stability in the prior art. Meanwhile, the structural characteristics of the compound, such as rich energetic ligands, as well as the alternately arranged oxidizing energetic anions and reducing organic cations in the space, endow the compound with excellent performance on instantaneously releasing energy at detonation. The resulting three-dimensional structure allows the compound to not only have an energetic material effect but also overcome shortcomings of some existing energetic materials.

PHARMACEUTICALLY ACCEPTABLE SALTS OF FATTY ACIDS

The present disclosure provides pharmaceutically acceptable stable salt forms of 15-lipoxygenase products, such as 15-HETrE lysine salt, compositions comprising same and methods of making and using same. 1. A salt of a 15-lipoxygenase product.2. The salt of claim 1 , wherein the salt is a pharmaceutically acceptable salt.3. The salt of claim 1 , wherein the salt comprises a lysine salt of the 15-lipoxygenase product.4. The salt of claim 1 , wherein the salt comprises a sodium salt of the 15-lipoxygenase product.5. The salt of claim 1 , wherein the salt comprises an ornithine salt of the 15-lipoxygenase product.6. The salt of claim 1 , wherein the salt comprises a piperazine salt of the 15-lipoxygenase product.7. The salt of claim 1 , wherein the salt comprises a meglumine salt of the 15-lipoxygenase product.8. The salt of further comprising the 15-lipoxygenase product in free acid form.9. The salt of claim 1 , wherein the salt is selected from the group consisting of: sodium claim 1 , lysine claim 1 , ornithine claim 1 , piperazine claim 1 , meglumine claim 1 , and combinations thereof.10. The salt of claim 1 , wherein the 15-lipoxygenase product is selected from the group consisting of: 13-HODE claim 1 , 15-HETrE claim 1 , 15-OHEPA claim 1 , 15-HETE claim 1 , and combinations thereof.11. 15-Hydroxy-5 claim 1 , 8 claim 1 ,11 claim 1 ,13-eicosatetraenoic acid lysine salt.12. A pharmaceutical composition comprising a salt form of a 15-lipoxygenase product.13. The pharmaceutical composition of further comprising an excipient.14. The pharmaceutical composition of claim 12 , wherein after storage for at least about 4 weeks claim 12 , the pharmaceutical composition comprises at least about 98% claim 12 , at least about 99% claim 12 , or about 100% of an initial amount of the salt form of the 15-lipoxygenase product.15. The pharmaceutical composition of claim 12 , wherein after storage for at least about 10 weeks or at least 24 weeks claim 12 , the pharmaceutical ...

Pharmaceutically Acceptable Salts of Fatty Acids

The present disclosure provides pharmaceutically acceptable stable salt forms of 15-lipoxygenase products, such as 15-HETrE lysine salt, compositions comprising same and methods of making and using same. 1. A salt of a 15-lipoxygenase product.2. The salt of claim 1 , wherein the salt is a pharmaceutically acceptable salt.3. The salt of claim 1 , wherein the salt comprises a lysine salt of the 15-lipoxygenase product.4. The salt of claim 1 , wherein the salt comprises a sodium salt of the 15-lipoxygenase product.5. The salt of claim 1 , wherein the salt comprises an ornithine salt of the 15-lipoxygenase product.6. The salt of claim 1 , wherein the salt comprises a piperazine salt of the 15-lipoxygenase product.7. The salt of claim 1 , wherein the salt comprises a meglumine salt of the 15-lipoxygenase product.8. The salt of further comprising the 15-lipoxygenase product in free acid form.9. The salt of claim 1 , wherein the salt is selected from the group consisting of: sodium claim 1 , lysine claim 1 , ornithine claim 1 , piperazine claim 1 , meglumine claim 1 , and combinations thereof.10. The salt of claim 1 , wherein the 15-lipoxygenase product is selected from the group consisting of: 13-HODE claim 1 , 15-HETrE claim 1 , 15-OHEPA claim 1 , 15-HETE claim 1 , and combinations thereof.11. 15-Hydroxy-5 claim 1 ,8 claim 1 ,11 claim 1 ,13-eicosatetraenoic acid lysine salt.12. A pharmaceutical composition comprising a salt form of a 15-lipoxygenase product.13. The pharmaceutical composition of further comprising an excipient.14. The pharmaceutical composition of claim 12 , wherein after storage for at least about 4 weeks claim 12 , the pharmaceutical composition comprises at least about 98% claim 12 , at least about 99% claim 12 , or about 100% of an initial amount of the salt form of the 15-lipoxygenase product.15. The pharmaceutical composition of claim 12 , wherein after storage for at least about 10 weeks or at least 24 weeks claim 12 , the pharmaceutical ...

ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS

Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. 2. The morpholinium compound of having the Formula 3 claim 1 , wherein X is hydroxide.3. The morpholinium compound of having the Formula 3 claim 1 , wherein R-Rare H.4. The morpholinium compound of having the Formula 1 wherein Rand Rform the cyclic alkyl group claim 3 , or having the Formula 4 wherein at least one of Rand Ris the alkyl group having the formula CH.5. The morpholinium compound of having the Formula 3 claim 1 , wherein at least one of R-Ris the alkyl group.6. The morpholinium compound of having the Formula 1 wherein Rand Rform the cyclic alkyl group claim 5 , or having the Formula 4 wherein at least one of Rand Ris the alkyl group having the formula CH.7. The morpholinium compound of having the Formula 1 wherein m is 5 claim 1 , R-Rare H claim 1 , and X is a halide.8. The morpholinium compound of having the Formula 2 wherein x is 1 claim 1 , and y is m.9. The morpholinium compound of having the Formula 3 wherein when Ris the alkyl group claim 1 , X is hydroxide.10. The morpholinium compound of having the Formula 2 wherein Ris the alkyl group and n is 1 claim 1 , m is 4 claim 1 , x is 1 claim 1 , and y is 4.11. The morpholinium compound of having the Formula 3 claim 1 , wherein at least two of R-Rare the alkyl group claim 1 , and wherein the at least two of R-Rare Rand R claim 1 , or Rand R claim 1 , or Rand R claim 1 , or Rand R.12. The morpholinium compound of having the Formula 4 wherein at least two of R-Rare the alkyl group claim 1 , and wherein at least one of Rand Ris the alkyl group having the formula CH claim 1 , or the Formula 1 wherein Rand Rform the cyclic alkyl group.13. The morpholinium compound of ...

DECARBOXYLATIVE CROSS-COUPLING AND APPLICATIONS THEREOF

Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. For example, methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound. 1. A method of cross-coupling comprising:providing a substrate including a carboxyl group;oxidizing the carboxyl group via a single electron transfer process, wherein the substrate subsequently undergoes decarboxylation to provide a substrate radical; andforming a C—C bond between the substrate radical and a coupling partner selected from the group consisting of a substituted aromatic compound and substituted aliphatic compound.2. The method of claim 1 , wherein the substrate is an aliphatic carboxylic acid.3. The method of claim 1 , wherein the aliphatic carboxylic acid is an amino acid.4. The method of claim 1 , wherein the aliphatic carboxylic acid is a fatty acid.5. The method of claim 1 , wherein the aliphatic carboxylic acid is of formula R—COH claim 1 , wherein Ris selected from the group consisting of -alkyl claim 1 , -cycloalkyl claim 1 , -heteroalkyl claim 1 , -heterocycloalkyl claim 1 , -alkenyl claim 1 , -cycloalkenyl claim 1 , -heteroalkenyl claim 1 , -heterocycloalkenyl claim 1 , -alkynyl claim 1 , -alkyl-aryl claim 1 , -alkyl-heteroaryl claim 1 , -alkyl-alkoxy claim 1 , -alkenyl-aryl claim 1 , - ...

Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. 1. An atorvastatin ammonium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 7.8 , 8.8 , 9.3 , 9.9 , 10.6 , 12.4 , and 19.5.2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. An atorvastatin erbumine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 5.4 , 7.3 , 9.5 , 17.8 , 19.2 , 20.0 , 22.2 , and 24.2 , or a solid state F nuclear magnetic resonance having the following chemical shifts expressed in parts per million: −110.4.10. An atorvastatin L-lysine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 6.7 , 9.8 , 17.1 , and 24.0.11. (canceled)12. (canceled)13. An atorvastatin piperazine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 7.8 , 9.3 , 11.8 , 16.1 , and 19.7.14. An atorvastatin sodium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 3.4 , 4.9 , 7.6 , 8.0 , 9.9 , 18.9 , and 19.7.15. An atorvastatin 2-amino-2-methylpropan-1-ol or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 4.2 , 8.3 , 16.0 , 17.5 , 18.3 , 19.4 , and 19.7 , or a solid state F nuclear magnetic resonance having the following chemical ...

METHOD FOR COUPLING A FIRST COMPOUND TO A SECOND COMPOUND

The present disclosure describes a method of coupling a first compound to a second compound, the method comprising: providing the first compound having a fluorosulfonate substituent; providing the second compound comprising an amine; and reacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound. The present disclosure further describes a one-pot method for coupling a first compound to a second compound. 1. A method of coupling a first compound to a second compound , the method comprising:providing the first compound having a fluorosulfonate substituent, the first compound comprising an aryl or a heteroaryl group;providing the second compound comprising an amine; andreacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound.2. The method of claim 1 , wherein the reaction mixture further includes a ligand.3. The method of wherein the catalyst is generated in-situ from a palladium precatalyst.4. The method of wherein the catalyst is generated in-situ from a palladium precatalyst claim 3 , the palladium precatalyst is selected from the group consisting of: Palladium(II) acetate claim 3 , Palladium(II) chloride claim 3 , Dichlorobis(acetonitrile)palladium(II) claim 3 , Dichlorobis(benzonitrile)palladium(II) claim 3 , Allylpalladium chloride dimer claim 3 , Palladium(II) acetylacetonate claim 3 , Palladium(II) bromide claim 3 , Bis(dibenzylideneacetone)palladium(0) claim 3 , Bis(2-methylallyl)palladium chloride dimer claim 3 , Crotylpalladium chloride dimer claim 3 , Dichloro(1 claim 3 ,5-cyclooctadiene)palladium(II) claim 3 , Dichloro(norbornadiene)palladium(II) claim 3 , Palladium(II) ...

SALT FORMS OF [R-(R*,R*)]-2-(4-FLUOROPHENYL)-BETA,DELTA-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. 1. An atorvastatin ammonium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 7.8 , 8.8 , 9.3 , 9.9 , 10.6 , 12.4 , and 19.5.2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. An atorvastatin erbumine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 5.4 , 7.3 , 9.5 , 17.8 , 19.2 , 20.0 , 22.2 , and 24.2 , or a solid state F nuclear magnetic resonance having the following chemical shifts expressed in parts per million: −110.4.10. An atorvastatin L-lysine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKradiation: 6.7 , 9.8 , 17.1 , and 24.0.11. (canceled)12. (canceled)13. An atorvastatin piperazine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 7.8 , 9.3 , 11.8 , 16.1 , and 19.7.14. An atorvastatin sodium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 3.4 , 4.9 , 7.6 , 8.0 , 9.9 , 18.9 , and 19.7.15. (canceled) The present invention relates to novel salt forms of atorvastatin which is known by the chemical name [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, useful as pharmaceutical agents, to methods for their ...

PHARMACEUTICALLY ACCEPTABLE SALTS OF FATTY ACIDS

The present disclosure provides pharmaceutically acceptable stable salt forms of 15-lipoxygenase products, such as 15-HETrE lysine salt, compositions comprising same and methods of making and using same. 1. A salt of a 15-lipoxygenase product.2. The salt of claim 1 , wherein the salt is a pharmaceutically acceptable salt.3. The salt of claim 1 , wherein the salt comprises a lysine salt of the 15-lipoxygenase product.4. The salt of claim 1 , wherein the salt comprises a sodium salt of the 15-lipoxygenase product.5. The salt of claim 1 , wherein the salt comprises an ornithine salt of the 15-lipoxygenase product.6. The salt of claim 1 , wherein the salt comprises a piperazine salt of the 15-lipoxygenase product.7. The salt of claim 1 , wherein the salt comprises a meglumine salt of the 15-lipoxygenase product.8. The salt of further comprising the 15-lipoxygenase product in free acid form.9. The salt of claim 1 , wherein the salt is selected from the group consisting of: sodium claim 1 , lysine claim 1 , ornithine claim 1 , piperazine claim 1 , meglumine claim 1 , and combinations thereof.10. The salt of claim 1 , wherein the 15-lipoxygenase product is selected from the group consisting of: 13-HODE claim 1 , 15-HETrE claim 1 , 15-OHEPA claim 1 , 15-HETE claim 1 , and combinations thereof.11. 15-Hydroxy-5 claim 1 ,8 claim 1 ,11 claim 1 ,13-eicosatetraenoic acid lysine salt.12. A pharmaceutical composition comprising a salt form of a 15-lipoxygenase product.13. The pharmaceutical composition of further comprising an excipient.14. The pharmaceutical composition of claim 12 , wherein after storage for at least about 4 weeks claim 12 , the pharmaceutical composition comprises at least about 98% claim 12 , at least about 99% claim 12 , or about 100% of an initial amount of the salt form of the 15-lipoxygenase product.15. The pharmaceutical composition of claim 12 , wherein after storage for at least about 10 weeks or at least 24 weeks claim 12 , the pharmaceutical ...

METHOD FOR THE MANUFACTURING OF 2-(3-(ALKYL AND ALKENYL)MORPHOLINO)-ETHAN-1-OLS

The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyllmorpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c] [1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazo-lo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process. 115.-. (canceled) The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl or alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to intermediates including 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.The compound 2-(3-(4-propylheptyl)morpholino)ethan-1-ol (CAS 79874-76-3) having the INN name delmopinol was disclosed for the first time by Ferrosan in EP0038785 and has the molecular structure depicted below.Delmopinol is used in the treatment of gingivitis, prevention of plaque formation and for oral hygiene in general. It is an active component in mouth wash liquids and toothpaste for use in humans and is also used in the maintenance of oral health in animals as described in WO 2007/099302. Ferrosan in EP0038785 disclosed methods for the synthesis of 2-(3-alkylmorpholino)-ethan-1-ol derivatives and the use of their pharmaceutically acceptable salts for the treatment of the oral cavity. The described methods have several ...

SUBSTITUTED BENZYLAMINE COMPOUNDS, THEIR USE IN MEDICINE, AND IN PARTICULAR THE TREATMENT OF HEPATITIS C VIRUS (HCV) INFECTION

The invention provides compounds of the formula (6): 2. A compound according to claim 1 , or a salt claim 1 , N-oxide or tautomer thereof claim 1 , wherein A is CH and E is CH.3. A compound according to claim 1 , or a salt claim 1 , N-oxide or tautomer thereof claim 1 , wherein Ris hydrogen.4. A compound according to claim 1 , or a salt claim 1 , N-oxide or tautomer thereof claim 1 , wherein Ris selected from:{'sub': 1-8', '1-8, 'sup': '6', 'an acyclic Chydrocarbon group optionally substituted with one substituent R, wherein one carbon atom of the acyclic Chydrocarbon group may optionally be replaced by a heteroatom O; and'}{'sup': '7a', 'a monocyclic carbocyclic or heterocyclic group of 3, 4, 5 or 6 ring members, of which 0, 1 or 2 are heteroatom ring members selected from O and N, the carbocyclic or heterocyclic group being optionally substituted with one or two substituents R.'}5. A compound according to claim 4 , or a salt claim 4 , N-oxide or tautomer thereof claim 4 , wherein Ris ethyl.6. A compound according to claim 1 , or a salt claim 1 , N-oxide or tautomer thereof claim 1 , wherein Ris selected from hydrogen and a group Rwherein Ris selected from a Calkyl group optionally substituted with a substituent R; cyclohexyl substituted with a substituent R; pyridine optionally substituted with a substituent R; and tetrahydroisoquinoline; wherein the substituent Ris selected from hydroxy; C(═O)NRR; piperidine; pyrrole and imidazole.7. A compound according to claim 6 , or a salt claim 6 , N-oxide or tautomer thereof claim 6 , wherein Ris a group Rwherein Ris a Calkyl group optionally substituted with a substituent R; wherein the substituent Ris selected from hydroxy and C(═O)NRR.8. A compound according to claim 6 , or a salt claim 6 , N-oxide or tautomer thereof claim 6 , wherein Ris hydrogen.9. A compound according to claim 1 , or a salt claim 1 , N-oxide or tautomer thereof claim 1 , wherein Ris fluorine.10. A compound according to claim 1 , or a salt claim 1 , N ...

DUAL NAV1.2/5HT2a INHIBITORS FOR TREATING CNS DISORDERS

Compounds of formula I: 2. A compound according to wherein Q is an optionally substituted nitrogenous aliphatic monocycle chosen from pyrrolidine claim 1 , piperidine claim 1 , morpholine claim 1 , piperazine claim 1 , azepane claim 1 , oxazepane claim 1 , thiazapane and diazepane.34-. (canceled)5. A compound according to wherein Q is an optionally substituted nitrogenous aliphatic bicycle chosen from diazabicycloheptane and diazabicyclooctane.6. (canceled)7. A compound according to wherein Q is an optionally substituted nitrogenous aliphatic spirocycle chosen from diazaspiro[4.4]nonane and diazaspiro[4.5]decane.8. (canceled)9. A compound according to wherein Q is an optionally substituted nitrogenous aliphatic spirocycle chosen from oxazaspiro[3.4]octane claim 1 , oxazaspiro[3.4]octene claim 1 , azaspiro [4.4]nonane claim 1 , and oxazaspiro [4.5]decane.10. (canceled)13. A compound according to wherein Ris an optionally substituted monocycle chosen from benzene claim 1 , cyclohexane claim 1 , tetrahydropyridazine and tetrahydropyran.14. A compound according to wherein Ris an optionally substituted fused bicycle containing an aromatic 6-membered ring and a non-aromatic 5-membered ring.15. (canceled)17. A compound according to wherein Ris an optionally substituted fused bicycle containing an aromatic 6-membered ring and a non-aromatic 6-membered ring.18. (canceled)19. A compound according to wherein Ris an optionally substituted fused bicycle containing two aromatic 6-membered rings.20. (canceled)21. A compound according to wherein Ris an optionally substituted fused bicycle containing an aromatic 6-membered ring and a non-aromatic 7-membered ring.2226-. (canceled)27. A compound according to wherein Lis —O—CHCH(OH)CH—.2829-. (canceled)30. A compound according to wherein Lis —CH—.3132-. (canceled)33. A compound according to wherein Lis —CHCH—.3435-. (canceled)36. A compound according to wherein Lis —OCHCH—.37. (canceled)38. A compound according to wherein Ris chosen ...

METHOD FOR COUPLING A FIRST COMPOUND TO A SECOND COMPOUND

The present disclosure describes a method of coupling a first compound to a second compound, the method comprising: providing the first compound having a fluorosulfonate substituent; providing the second compound comprising an amine; and reacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound. The present disclosure further describes a one-pot method for coupling a first compound to a second compound. 1. A method of coupling a first compound to a second compound , the method comprising:{'sub': '2', 'providing the first compound having a fluorosulfonate substituent substituent of the formula —OSOF, the first compound comprising an aryl or a heteroaryl group;'}providing the second compound comprising an amine; andreacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound.2. The method of claim 1 , wherein the reaction mixture further includes a ligand.3. The method of wherein the catalyst is generated in-situ from a palladium precatalyst.4. The method of wherein the catalyst is generated in-situ from a palladium precatalyst claim 1 , the palladium precatalyst is selected from the group consisting of: Palladium(II) acetate claim 1 , Palladium(II) chloride claim 1 , Dichlorobis(acetonitrile)palladium(II) claim 1 , Dichlorobis(benzonitrile)palladium(II) claim 1 , Allylpalladium chloride dimer claim 1 , Palladium(II) acetylacetonate claim 1 , Palladium(II) bromideBis(dibenzylideneacetone)palladium(0) claim 1 , Bis(2-methylallyl)palladium chloride dimer claim 1 , Crotylpalladium chloride dimer claim 1 , Dichloro(1 claim 1 ,5-cyclooctadiene)palladium(II) claim 1 , Dichloro(norbornadiene) ...

Silicon-based cross coupling agents and methods of their use

Compositions and methods using silicon-based cross-coupling agents in the formation of carbon-carbon and carbon-nitrogen bonds are described.

HYDROGEN SULFIDE DONOR IN ORGANIC SALT FORM AND PREPARATION METHOD THEREFOR

A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value. 1. A hydrogen sulfide donor in organic salt form , characterized in that the donor is a salt structure formed by organic compounds with basic moiety and hydrogen sulfide.2. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those pharmacological compounds possessing physiological and/or pharmacological activities.3. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those with the structures selected from the group consisting of guanidines claim 1 , amidines claim 1 , hydrazines.4. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those amino acid compounds such as arginine claim 1 , lysine claim 1 , etc.5. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are alkaloids.6. A preparative method for hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are dissolved in the solvent claim 1 , to which is added hydrogen sulfide ...

Apparatus and Process for the Automated Chemical Synthesis of Compounds

Provided is an apparatus for the automated synthesis of at least one chemical compound including: at least one cartridge including at least one first compartment for providing at least one first reagent for the chemical synthesis of the at least one compound; at least one second compartment for providing at least one second reagent for the chemical synthesis of the at least one compound, and at least one third compartment for purifying the at least one synthesized compound; at least one reaction container for providing the compounds to be fed into at least one of the compartments of the cartridge and/or collecting the reaction product from at least one of the compartments of the cartridge; at least one solvent container; at least two flow patch selecting valve and at least one pump. 1. An apparatus for the automated synthesis of at least one chemical compound , comprising:at least one cartridge comprising:at least one first compartment for providing at least one first reagent for the chemical synthesis of the at least one compound;at least one second compartment for providing at least one second reagent for the chemical synthesis of the at least one compound, andat least one third compartment for purifying the at least one synthesized compound;at least one reaction container for providing the compounds to be fed into at least one of the compartments of the cartridge and/or collecting the reaction product from at least one of the compartments of the cartridge;at least one solvent container for storing solvent systems used for at least one of the compartments of the cartridge;optionally at least one waste container for collecting the waste from at least one of the compartments of the cartridge;at least two flow patch selecting valves, wherein at least one first valve selects the liquid source and at least one second valve directs the liquid to one of the compartments in the cartridge, reaction container or optional waste container, andat least one pump arranged ...

1,4-Disubstituted Piperidines, 1,4-Disubstituted Piperazines, 1,4-Disubstituted Diazepines, and 1,3-Disubstituted Pyrrolidine Compounds

The present invention is directed to 1,4-disubstituted piperidines, 1,4-disubstituted piperazines, 1,4-disubstituted diazepanes, and 1,3-disubstituted pyrrolidine compounds and their use.

PVC Plasticizers and Methods for Making Thereof

A plasticized PVC composition free of phthalate is disclosed. The composition comprises a tertiary diamide plasticizer prepared from biorenewable feedstock such as fatty acid selected from tall oil fatty acids, tall oil fatty acid monomers, fatty acids derived from tall oil fatty acid, and mixtures thereof. The tertiary diamide plasticizer is a reaction product of a reactant mixture comprising the fatty acid and one or more monocyclic diamines.

Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. 1. An atorvastatin ammonium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 7.8 , 8.8 , 9.3 , 9.9 , 10.6 , 12.4 , and 19.5.2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. An atorvastatin erbumine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 5.4 , 7.3 , 9.5 , 17.8 , 19.2 , 20.0 , 22.2 , and 24.2 , or a solid state F nuclear magnetic resonance having the following chemical shifts expressed in parts per million: −110.4.10. An atorvastatin L-lysine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 6.7 , 9.8 , 17.1 , and 24.0.11. (canceled)12. An atorvastatin olamine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 8.5 , 9.8 , 17.4 , 18.6 , 20.9 , 22.5 , and 24.1 , or a solid state F nuclear magnetic resonance having the following chemical shifts measured in parts per million: −118.7.13. An atorvastatin piperazine or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 7.8 , 9.3 , 11.8 , 16.1 , and 19.7.14. An atorvastatin sodium or hydrate thereof having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK radiation: 3.4 , 4.9 , 7.6 , 8.0 , 9.9 , 18 ...

Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Catalytic Hydrogenation for the Preparation of Amines from Amide Acetals, Ketene N,O-Acetals or Ester Imides

The present invention relates to a process for the preparation of amines, comprising the following steps: Reaction of a (i) amide acetal of the general formula (I), or (ii) ketene N,O-acetal of the general formula (II), or (iii) ester imide of the general formula (III) with H 2 in the presence of a hydrogenation catalyst, where catalyst and amide acetal or ketene N,O-acetal or ester imide are used in a molar ratio of from 1:10 to 1:100 000 and where a hydrogen pressure of from 0.1 bar to 200 bar is established and where a temperature in the range of from 0° C. to 250° C. is established.

PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS

Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained. 1. A morpholinium compound comprising: {'chemistry': {'@id': 'CHEM-US-00001', '@num': '00001', 'img': {'@id': 'EMI-C00001', '@he': '19.47mm', '@wi': '31.24mm', '@file': 'US20180258058A1-20180913-C00001.TIF', '@alt': 'embedded image', '@img-content': 'chem', '@img-format': 'tif'}}, 'br': None, 'sub': 1', '2', '3', '4', '9', '10', '5', '6', '7', '8, 'sup': +', '−, '2-R-2-R-3-R-3-R-4-R-4-R-5-R-5-R-6-R-6-R-1-oxa-4-azoniumcyclohexane-X,\u2003\u2003Formula 1, 'a 1-oxa-4-azonium cyclohexane salt having a structure of{'sub': 1', '9', 'n', '2n+1', '10', 'n', '2n+1', 'p', '2p−1, 'wherein R-Rare independently selected from H or an alkyl group having the formula CH, Ris selected from an alkyl group having the formula CHwhere n is in the range from 1 to 4, benzyl, 1-methylnaphthalene, 2-methylnaphthalene and a non-olefinic alkyl group having the formula CHwhere p is in the range from 4 to 10, X is halide or hydroxide, and the total number of C atoms in the molecule is in the range of 4 to 16;'}or combinations thereof.2. The morpholinium compound of wherein X is hydroxide.3. The morpholinium compound of wherein R-Rare H.4. The morpholinium compound of wherein at least one of Rand Ris the alkyl group having the formula CH.5. The morpholinium compound of wherein at least one of R-Ris an alkyl group.6. The morpholinium compound of wherein at least one of Rand Ris an alkyl group having the formula CH.7. The morpholinium ...

Synthesis of a Monoacylglycerol Lipase Inhibitor

Described herein is the manufacture of MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate including salts thereof. 1. A process for the manufacture of 1 ,1 ,1 ,3 ,3 ,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate comprising the steps of:a) reacting tert-butyl piperazine-1-carboxylate with hexafluoropropan-2-ol in the presence of an acyl transfer agent to form 1-(tert-butyl) 4-(1,1,1,3,3,3-hexafluoropropan-2-yl) piperazine-1,4-dicarboxylate, wherein step a) is carried out in a first solvent;b) reacting 1-(tert-butyl) 4-(1,1,1,3,3,3-hexafluoropropan-2-yl) piperazine-1,4-dicarboxylate obtained in step a) with a strong acid to form 1,1,1,3,3,3-hexafluoropropan-2-yl piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof, wherein step b) is optionally carried out in a second solvent;c) reacting 1,1,1,3,3,3-hexafluoropropan-2-yl piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof obtained in step b) with 2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzaldehyde in the presence of a reducing agent and an organic base to form a reaction mixture comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, wherein the reaction in step c) is carried out in a third solvent.2. The process according to claim 1 , wherein step a) is carried out under pressure of 2 bar to 6 bar.3. The process according to claim 1 , wherein the ingredients in step a) are added in the consecutive order of the acyl transfer agent claim 1 , the first solvent claim 1 , tert-butyl piperazine-1-carboxylate claim 1 , and hexafluoropropan-2-ol as the last ingredient.4. The process according to claim 1 , wherein the strong acid in step b) is HCl; and wherein the step b) is carried out in a second solvent.5. The process according to claim 4 , wherein the second solvent is selected from the group ...

Catalytic Hydrogenation for Producing Amines from Carboxylic Acid Amides, Carboxylic Acid Diamides, Di-, Tri-, or Polypeptides, or Peptide Amides

The present invention relates to a process for the preparation of amines, comprising the following steps: a. reaction of a (i) carboxylic acid amide of the general formula (I), or (ii) carboxylic acid diamide of the general formula (II), or (iii) di-, tri- or polypeptide, or (iv) peptide amide with carboxy-terminal amide function with an alkylating agent, b. addition of a hydrogenation catalyst to the reaction mixture in a molar ratio of from 1:10 to 1:100 000, based on carboxylic acid amide, carboxylic acid diamide, di-, tri- or polypeptide or peptide amide, c. reaction of the reaction mixture with hydrogen, where a hydrogen pressure of from 0.1 bar to 200 bar is established and where a temperature in a range of from 0° C. to 250° C. is established. 110-. (canceled)12. The process of claim 11 , wherein the alkylating agent is selected from the group consisting of: alkyl halides; esters of sulphonic acid; esters of fluorosulphonic acid; esters of trifluoromethanesulphonic acid; esters of chloroformic acid; oxonium salts; dialkyl sulphates; and diazomethane.13. The process of claim 11 , wherein the hydrogenation catalyst comprises at least one active metal.14. The process of claim 13 , wherein the active metal is a metal of group VII B and/or VIII B of the Periodic Table of the Elements.15. The process of claim 11 , wherein claim 11 , after step a) claim 11 , a base is added to the reaction mixture and wherein a molar ratio of base to alkylating agent of from 1:1 to 1:3 is produced.16. The process of claim 11 , wherein the reaction is carried out in a solvent.17. The process of claim 16 , wherein the solvent is selected from the group consisting of: hydrocarbons; chlorinated hydrocarbons; ethers; esters; and alcohols.18. The process of claim 11 , wherein the reaction is carried out without solvents.19. The process of claim 16 , wherein said alkylating agent is anhydrous and is selected from the group consisting of: carboxylic acid amide; carboxylic acid diamide; a di ...

ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS

Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained. 1. A morpholinium compound comprising a 1-oxa-4-azonium cyclohexane salt having a structure of:{'chemistry': {'@id': 'CHEM-US-00001', '@num': '00001', 'img': {'@id': 'EMI-C00001', '@he': '25.91mm', '@wi': '61.64mm', '@file': 'US20180265485A1-20180920-C00001.TIF', '@alt': 'embedded image', '@img-content': 'chem', '@img-format': 'tif'}}, 'br': None, 'sub': 1', '2', '3', '4', '9', '10', '5', '6', '7', '8, 'sup': +', '−, '2-R-2-R-3-R-3-R-4-R-4-R-5-R-5-R-6-R-6-R-1-oxa-4-azoniumcyclohexane-X,'}{'sub': 1', '8', 'n', '2n+1', '1', '8', '9', '10', 'm', '2m, 'wherein R-Rare independently selected from H or an alkyl group having the formula CHwhere n is in the range from 1 to 4; at least one of R-Ris an alkyl group; Rand Rform a cyclic alkyl group having the formula CHforming a heterocycle of ring size q, where m is in the range from 4 to 8, and q is in the range of 5 to m+1; X is hydroxide; and the total number of C atoms in the molecule is in a range of 8 to 17.'}2. The morpholinium compound of having the Formula 1 claim 1 , wherein at least two of R-Rare an alkyl group.3. The morpholinium compound of having the Formula 1 claim 1 , wherein at least two of R-Rare an alkyl group claim 1 , and wherein at least two of R-Rare the same alkyl group.4. The morpholinium compound of having the Formula 1 claim 1 , wherein the at least two of R-Rare Rand R claim 1 , or Rand R claim 1 , or Rand R claim 1 , or Rand R.5. A ...

ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS

Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained. 2. The morpholinium compound of wherein X is hydroxide.3. The morpholinium compound of wherein R-Rare H.4. The morpholinium compound of wherein at least one of R-Ris an alkyl group.5. The morpholinium compound of wherein x is 1 claim 1 , and y is m.6. The morpholinium compound of wherein when Ris an alkyl group and X is hydroxide.7. The morpholinium compound of wherein Ris an alkyl group and n is 1 claim 1 , m is 4 claim 1 , x is 1 claim 1 , and y is 4.8. The morpholinium compound of wherein at least two of R-Rare the alkyl group claim 1 , and wherein the at least two of R-Rare Rand R claim 1 , or Rand R claim 1 , or Rand R claim 1 , or Rand R.9. The morpholinium compound of wherein at least two of R-Rare an alkyl group claim 1 , and wherein at least two of R-Rare the same alkyl group.10. A method for synthesizing a 1-oxa-4-azonium cyclohexane salt claim 1 , comprising:preparing an aqueous mixture comprising water, a substituted hydrocarbon, and a 1-oxa-4-azacyclohexane derivative;reacting the aqueous mixture;obtaining a solution comprising the 1-oxa-4-azonium cyclohexane salt; andwherein the mixture and the solution are essentially free of aluminum and silicon. This application is a Continuation-In-Part of copending U.S. application Ser. No. 15/334,154 filed Oct. 25, 2016, which application is a Division of U.S. application Ser. No. 14/561,132 filed Dec. 4, 2014, now U.S. Pat. No. 9,522,896 issued Dec. 20 ...

NOVEL RUTHENIUM COMPLEXES AND THEIR USES IN PROCESSES FOR FORMATION AND/OR HYDROGENATION OF ESTERS, AMIDES AND DERIVATIVES THEREOF

The present invention relates to novel Ruthenium complexes and related borohydride complexes, and their use for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including preparing polyamides (e.g., polypeptides) by reacting dialcohols and diamines or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones), cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to novel uses of certain pyridine Ruthenium complexes. 181.-. (canceled)85. The borane derivative according to claim 82 , wherein Xand/or Xare absent claim 82 , and the pyridyl or bipyridyl moiety is unsubstituted.86. The borane derivative according to claim 82 , wherein Lis phosphine (PRR).87. A process for hydrogenating an amide to an alcohol and an amine claim 82 , comprising the step of reacting the amide with molecular hydrogen (H) in the presence of the borane derivative according to .88. A process for hydrogenating an ester claim 84 , organic carbonate claim 84 , carbamate or urea derivative claim 84 , comprising the step of reacting the ester claim 84 , organic carbonate claim 84 , carbamate or urea derivative with molecular hydrogen (H) in the presence of the borane derivative according to claim 84 , thereby hydrogenating the ester claim 84 , organic carbonate claim 84 , carbamate or urea derivative and generating at least ...

4-(p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinoly)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

PROCESS FOR THE DISTILLATION OF A MIXTURE COMPRISING A CYCLIC N-VINYLAMIDE

A process for the distillation of a mixture which consists to at least 90% by weight of a cyclic N-vinylamide and which comprises a stabilizer, wherein 1. A process for the distillation of a mixture comprising a stabilizer and at least 90% by weight of a cyclic N-vinylamide , the method comprising:adding a polyether to the mixture before or during distillation to obtain a product comprising at least 99.5% by weight of the cyclic N-vinylamide.2. The process according to claim 1 , wherein the cyclic N-vinylamide is N-vinylpyrrolidone (NVP).3. The process according to claim 1 , wherein the mixture comprises at least 98% by weight of the cyclic N-vinylamide.4. The process according to claim 1 , wherein the stabilizer is a phenol or amine type polymerization inhibitor.5. The process according to claim 1 , wherein the stabilizer is a N claim 1 ,N′-di-alkyl-p-phenylendiamine.6. The process according to claim 1 , wherein the mixture comprises from 3 to 500 ppm of the stabilizer.7. The process according to claim 1 , wherein the polyether is a polyether of formula I{'br': None, 'sub': 1', 'n', '2, 'RO—(X—O—)R'}{'sub': 1', '2', '2', '6, 'wherein Rand Rare each independently hydrogen or a hydrocarbon group with 1 to 10 C atoms, X is a straight-chain or branched C-Calkylene group and n is an integer of from 2 to 100.'}8. The process according to claim 7 , wherein X is an ethylene or propylene group or a mixture thereof.9. The process according to claim 7 , wherein Rand Rin formula I are each independently hydrogen or an alkyl group with 1 to 3 C atoms.10. The process according to claim 7 , wherein Rand Rin formula I are each hydrogen.11. The process according to claim 7 , wherein n is an integer of from 2 to 50.12. The process according to claim 1 , wherein the process is performed in a distillation device comprising a distillation column or an evaporator and the mixture is continuously fed to the distillation device.13. The process according to claim 12 , wherein the polyether ...

Synergistic compositions

The present invention describes a synergistic composition comprising of one or more statins, or one or more dipeptidyl peptidase IV (DPP IV) inhibitor or one or more biguanide antihyperglycaemic agent and a PPAR agonist of formula (Ia) for the treatment of diabetes, especially non-insulin dependent diabetes (NIDDM) or Type 2 diabetes and conditions associated with diabetes mellitus and to compositions suitable for use in such method. The invention also describes the preparation of such compositions. The present invention also relates to certain novel salts of the PPAR agonist of formula (I), processes for the preparation of these novel salts and use thereof.

SYNERGISTIC COMPOSITIONS

The present invention describes a synergistic composition comprising of one or more statins, or one or more dipeptidyl peptidase IV (DPP IV) inhibitor or one or more biguanide antihyperglycaemic agent and a PPAR agonist of formula (1a) for the treatment of diabetes, especially non-insulin dependent diabetes or Type 2 diabetes and conditions associated with diabetes mellitus and to compositions suitable for use in such method. The invention also describes the preparation of such compositions. The present invention also relates to certain novel salts of the PPAR agonist of formula (I), processes for the preparation of: these novel salts and use thereof.

Bioconjugation of Polypeptides

Certain embodiments of the present invention relate to methods of forming and manipulating bioconjugates. Particularly, but not exclusively certain embodiments relate to methods of reversible carbon-carbon bond bioconjugation using aldol based chemical reactions at physiological conditions. 169-. (canceled)71. A method according to claim 70 , wherein the catalyst molecule comprises a secondary amine moiety or an acid addition salt thereof.72. A method according to claim 71 , wherein the catalyst molecule comprises a cyclic secondary amine molecule.74. A method according to claim 72 , wherein the catalyst molecule comprises a substituted cyclic secondary amine molecule claim 72 , wherein optionally the substituted cyclic secondary amine molecule is substituted pyrrolidine or wherein the catalyst molecule comprises a tetrazole-substituted cyclic molecule claim 72 , wherein optionally the tetrazole-substituted cyclic molecule is pyrrolidine substituted with tetrazole e.g. 2S-tetrazolylpyrrolidine.75. The method according to claim 70 , which comprises contacting the first polypeptide claim 70 , the aldehyde donor molecule and the catalyst molecule in a buffer solution having a pH of between about 7 and 8 and/or at a temperature of between about 35° C. and about 38° C.76. The method according to claim 70 , wherein the first polypeptide comprises the first aldehyde moiety at an internal sequence of the first polypeptide; at a terminal loop claim 70 , a C-terminus claim 70 , or an N-terminus of the first polypeptide; on a solvent-accessible region of the first polypeptide when folded; and/or at a site of post-translational modification of the first polypeptide that is native or non-native to the amino acid sequence of the first polypeptide.77. The method according to claim 70 , wherein the aldehyde donor moiety further comprises a functional moiety and the method comprises incorporating the functional moiety into the second polypeptide.78. The method according to claim 77 ...

Base generator, reagent, organic salt, composition, method for manufacturing device, cured film and device

A curing agent or a curing accelerator which is easy to synthesize and may cure an epoxy resin and the like, or may accelerate the curing is provided. A curing agent or a curing accelerator according to some embodiments of the present invention has a highly-coordinated silicon structure.

METHOD FOR THE MANUFACTURING OF 2-(3-(ALKYL AND ALKENYL)MORPHOLINO)-ETHAN-1-OLS

The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process. 3. The process according to claim 2 , wherein compound (II′) is 8a-4-propylhept-3-en-1-yl-hexahydrooxazolo[2 claim 2 ,3-c][1 claim 2 ,4]oxazine and said reduction in step iii) is performed by catalytic hydrogenation.4. The process according to claim 2 , wherein compound (II′) is 8a-4-propylheptyl-hexahydrooxazolo[2 claim 2 ,3-c][1 claim 2 ,4]oxazine and said reduction in step iii) is performed by catalytic hydrogenation or by treatment with a metal borohydride.5. The process according to wherein compound (II′) is 8a-4-propylhept-3-en-1-yl-hexahydrooxazolo[2 claim 2 ,3-c][1 claim 2 ,4]oxazine and said reduction in step iii) proceeds through 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol.6. The process according to claim 1 , wherein X is selected from the group consisting of Cl and Br.7. The process according to claim 1 , wherein said strong base used in step i) is selected from the group consisting of metal hydrides claim 1 , metal alkoxides claim 1 , metal amides claim 1 , organolithium reagents and organomagnesium reagents.8. The process according to claim 7 , wherein said strong base is lithium hydride9. The process according to claim 1 , wherein said strong base in step i) is used in 0.95-1.05 molar equivalents relative to 4-(2-hydroxyethyl)morpholin-3-one.10. The process according to claim 1 , wherein the reaction in step ii) is performed at a temperature of − ...

METHOD FOR THE CONTINUOUS SEPARATION BY DISTILLATION OF MIXTURES THAT CONTAIN MORPHOLINE (MO), MONOAMINODIGLYCOL (ADG), AMMONIA, WATER AND METHOXYETHANOL (MOE)

A process for the continuous distillative separation of mixtures comprising morpholine (MO), monoaminodiglycol (ADG), ammonia, water and methoxyethanol (MOE), obtained by reacting diethylene glycol (DEG) with ammonia, wherein ammonia, water, ADG and DEG are removed by distillation and the resulting stream comprising MO and MOE is supplied to a distillation column K in which at a top pressure of from 20 to 2000 mbar MO, MOE and organic products having a boiling point 128° C. (1.013 bar) are removed via the bottom and organic products having a boiling point 128° C. are removed overhead, and also MO is removed via a side draw, where K is equipped with an evaporator for heating the bottoms, into which is fed heating vapor having a pressure of from 1 to 10 bar. 14040. A process for the continuous distillative separation of mixtures comprising morpholine (MO) , monoaminodiglycol (ADG) , ammonia , water and methoxyethanol (MOE) , obtained by reacting diethylene glycol (DEG) with ammonia , wherein ammonia , water , ADG and DEG are removed by distillation and the resulting stream comprising MO and MOE is supplied to a distillation column K in which at a top pressure of from 20 to 2000 mbar MO , MOE and organic products having a boiling point ≥128° C. (1.013 bar) are removed via the bottom and organic products having a boiling point ≤128° C. are removed overhead , and also MO is removed via a side draw , where K is equipped with an evaporator for heating the bottoms , into which is fed heating vapor having a pressure of from 1 to 10 bar.2101020. The process according to claim 1 , wherein claim 1 , for the distillative removal of ammonia claim 1 , water claim 1 , ADG and DEG claim 1 , the ammonia is removed overhead in a first distillation column K claim 1 , the bottoms output from K is supplied to a second distillation column K claim 1 , in which water and organic products are removed overhead at a top temperature of from 45 to 198° C. and a top pressure of from 0.1 to 15 bar ...

Method for depleting 2-methoxyethanol (moe)

A process for the depletion of 2-methoxyethanol (MOE) from a mixture comprising predominantly morpholine (MO) (crude morpholine), wherein crude morpholine is distilled in a distillation column in the presence of an alkali metal compound of the general formula M + [RO − ] (M + is alkali metal cation and R is hydrogen (H), methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl), where MO and a compound of the general formula R—OH are distilled off and an alkali metal methoxyethoxide of the general formula M + [MeOEtO − ] is obtained in the bottom of the column.

Piperazine derivative

A piperazine derivative represented by the formula (1):    wherein n is an integer of 1 to 8; R 1 represents hydrogen or C 1-10 alkyl; A represents CH or nitrogen; Ar 1 represents phenyl or substituted phenyl; and Y represents a group represented by the formula Y 1 -Y 2 -Ar 2 or Y 3 -Y 4 (Ar 5 )-Ar 6 or a pharmaceutically acceptable salt of the derivative. The novel piperazine derivative has MC4 receptor antagonistic activity.

Catalyst system comprising transition metal and imidazoline-2-ylidene or imidazolidine-2-ylidene

This invention provides a catalyst system useful in many coupling reactions, such as Suzuki, Kumada, Heck, and amination reactions. The catalyst system of the present invention makes use of N-heterocyclic carbenes or their protonated salts. The composition of the catalyst system comprises at least one transition metal compound and at least one N-heterocyclic carbene or its protonated salt. This invention further provides novel N-heterocyclic carbenes and their protonated salts. One type of N-heterocyclic carbene used in this invention is an imidazolinc-2-ylidene wherein the 1 and 3 positions are each, independently, substituted by an aromatic group in which each ortho position is, independently, substituted by a secondary or tertiary group which has at least three atoms.

Use a catalyst system comprising nickel palladium or platinum and imidazoline-2-ylidene or imidazolidine-2-ylidene in stille coupling reactions

This invention provides a process for conducting Stille coupling reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in Stille couplings of aryl halides. A Stille coupling can be carried out by mixing, in a liquid medium, at least one strong base; at least one aryl halide or aryl pseudohalide in which all substituents are other than stannyl groups, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one halogen atom selected from the group consisting of a chlorine atom, a bromine atom, and an iodine atom; at least one organotin compound wherein the tin atom is quaternary, wherein one group bound to the tin atom is unsaturated at the alpha or beta position, and wherein each of the remaining groups bound to the tin atom is a saturated group; at least one metal compound comprising at least one metal atom selected from nickel, palladium, and platinum, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene. One preferred type of N-heterocyclic carbene is an imidazoline-2-ylidene of the formula wherein R 1 and R 2 are each, independently, alkyl or aryl groups having at least 3 carbon atoms, R 3 and R 4 are each, independently, a hydrogen atom, a halogen atom, or a hydrocarbyl group.

Use of a catalyst system comprising nickel, palladium, or platinum and imidazoline-2-ylidene or imidazolidine-2-ylidene in kumada coupling reactions

This invention provides a process for conducting Kumada coupling reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in Kumada couplings of aryl halides. A Kumada coupling can be carried out by mixing, in a liquid medium, at least one aryl halide, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one halogen atom selected from the group consisting of a chlorine atom, a bromine atom, and an iodine atom; at least one Grignard reagent; at least one metal compound comprising at least one metal atom selected from nickel, palladium, and platinum, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene. One preferred type of N-heterocyclic carbene is an imidazoline-2-ylidene of the formula wherein R 1 and R 2 are each, independently, alkyl or aryl groups having at least 3 carbon atoms, R 3 and R 4 are each, independently, a hydrogen atom, a halogen atom, or a hydrocarbyl group. Homocoupling of aryl pseudohalides is also feasible using the processes of this invention.

Use of catalyst system comprising nickel, palladium, or platinum and imidazoline-2-ylidene or imidazolidine-2-ylidene in amination reactions

This invention provides a process for conducting amination reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in aminations of aryl halides and aryl pseudohalides. An amination can be carried out by mixing, in a liquid medium, at least one strong base; at least one aryl halide or aryl pseudohalide in which all substituents are other than amino groups, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one halogen atom selected from the group consisting of a chlorine atom, a bromine atom, and an iodine atom; at least one primary amine and/or at least one secondary amine; at least one metal compound comprising at least one metal atom selected from nickel, palladium, and platinum, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene. One preferred type of N-heterocyclic carbene is an imidazoline-2-ylidene of the formula wherein R 1 and R 2 are each, independently, alkyl or aryl groups having at least 3 carbon atoms, R 3 and R 4 are each, independently, a hydrogen atom, a halogen atom, or a hydrocarbyl group.

Catalyzed coupling reactions of aryl halides with silanes

A process for conducting coupling reactions of aryl halides with unsaturated silanes is described. The processes use N-heterocyclic carbenes as ancillary ligands in these coupling reactions. A coupling of an aryl halide with an unsaturated silane can be carried out by mixing, in a liquid medium, at least one strong base; at least one aryl halide or aryl pseudohalide in which all substituents are other than silyl groups, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one chlorine atom, bromine atom, or iodine atom; at least one silane wherein the silicon atom is quaternary, wherein one group bound to the silicon atom is unsaturated at the alpha or beta position, and wherein each of the remaining groups bound to the silicon atom is a saturated hydrocarbyl or a saturated hydrocarbyloxy group; at least one nickel, palladium, or platinum compound, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene. One preferred type of N-heterocyclic carbene is an imidazoline-2-ylidene of the formula wherein R 1 and R 2 are each, independently, alkyl or aryl groups having at least 3 carbon atoms, R 3 and R 4 are each, independently, a hydrogen atom, a halogen atom, or a hydrocarbyl group.

Catalyst and method for producing an amine

The invention relates to a method for producing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound, selected from the group containing ammonia and primary and secondary amines, in the presence of a supported catalyst that contains copper, nickel and cobalt. According to the invention, the catalytically active mass of the catalyst, prior to the reduction of the same using hydrogen, contains oxygen-containing compounds of aluminium, copper, nickel and cobalt and an amount ranging between 0.2 and 5.0 wt. % of oxygen-containing compounds of tin, calculated as SnO. The invention also relates to catalysts defined as above.

Method for producing an amine

The invention relates to a method for producing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound, selected from the group comprising ammonia, primary and secondary amines, in the presence of a zirconium dioxide and nickel-containing catalyst. The catalytically active mass of the catalyst, prior to its reduction with hydrogen, contains oxygen-containing compounds of zirconium, copper, nickel and cobalt and 5.5 to 12 wt% of oxygen-containing compounds of molybdenum, calculated as MoO3.

Synthesis of deuterated morpholine derivatives

The present invention is directed to a process for preparing a 2,26,6- d 4 -morpholine derivative represented by Structural Formula (I), or a salt thereof.

Ligands for metals and improved metal-catalyzed processes based thereon

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Ligands for metals and improved metal-catalyzed processes based thereon

One aspect of the present invention relates to novel, electron-rich bidentate ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Ligands for metals and improved metal-catalyzed processes based thereon

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Ligands for metals and improved metal-catalyzed processes based thereon

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

イオン液体および柔粘性結晶

本発明は、アニオンとカチオンから構成されるイオン液体又は柔粘性結晶であって、アニオンが［Ｃ（ＳＯ２Ｆ）３］−を含み、カチオンが1-エチル-3-メチルイミダゾリウム（［ＥＭＩ］＋）、N,N-ジエチル-N-メチル-(2-メトキシエチル)アンモニウム（［ＤＥＭＥ］＋）、N-メチル-N-プロピルピロリジニウム（［Ｐｙ１３］＋）、N-メチル-N-プロピルピペリジニウム（［ＰＰ１３］＋）、テトラメチルアンモニウム（［Ｎ１１１１］＋）、テトラエチルアンモニウム（［Ｎ２２２２］＋）、トリメチルヘキシルアンモニウム（［Ｎ６１１１］＋）、トリエチルヘキシルアンモニウム（［Ｎ６２２２］＋）、N-メチル-N-エチルピロリジニウム（［Ｐｙ１２］＋）、1-ブチル-3-メチルイミダゾリウム（［Ｃ４ｍｉｍ］＋）及び1-ヘキシル-3-メチルイミダゾリウム（［Ｃ６ｍｉｍ］＋）からなる群から選ばれる少なくとも１種を含む、イオン液体又は柔粘性結晶を提供するものである。

Substituted aminomethylphosphines, coordination complexes of aminomethylphosphines and their synthesis

Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.

Distillate fuel compositions having a hydrocarbon substituted alkylene polyamine

FUEL COMPOSITIONS HAVING POLYPROPYLENE OR POLYISOBUTYLENE SUBSTITUTED POLYAMINES AS DETERGENTS OR DISPERSANTS.

Benzene compound

Disclosed is a benzene compound represented by any one of general formulae (A) to (D).  The benzene compound can emit light efficiently in a solid state. (In general formula (A), RA 1 and RA 2 independently represent an amino group, or the like; RA 3 and RA 4 independently represent a lower alkyl group, or the like; RA 5 and RA 6 independently represent a lower alkyl group, or the like; RA 7 and RA 8 independently represent a lower alkyl group, or the like; and m and n independently represent an integer of 0 to 6.) (In general formula (B), RB 1 and RB 2 independently represent a lower alkyl group, or the like; RB 3 and RB 5 independently represent a halogen atom, or the like; and RB 4 represents a lower alkyl group, or the like.) (In general formula (C), RC 1 represents an electron-withdrawing group such as a halogen-substituted lower alkyl group; and RC 2 represents an electron-donating group such as an amino group, which may have a lower alkyl group.) (In general formula (D), RD 1 , RD 2 , RD 3 and RD 4 independently represent a hydrogen atom, or a halogen atom; and RD 5 represents a hydrogen atom, or an alkyl group.)

由甘油生产胺的方法

本发明涉及一种通过使甘油与氢气和选自氨、伯胺和仲胺的胺化剂在催化剂存在下在100-400℃的温度和0.01-40MPa(0.1-400巴)的压力下反应而生产胺的方法。优选使用基于可再生原料的甘油。催化剂优选包含一种或多种元素周期表第8和/或9和/或10和/或11族的金属或一种或多种其含氧化合物。本发明进一步涉及反应产物在水泥或混凝土生产中作为添加剂以及在其他应用领域中的用途。本发明进一步涉及化合物1，2，3-三氨基丙烷、2-氨基甲基-6-甲基哌嗪、2，5-二(氨基甲基)哌嗪和2，6-二(氨基甲基)哌嗪。

PROCESS FOR THE PRODUCTION OF 2 (3 ALCHILMORPHOLIN) -ETAN-1-OLO

Method of producing amines from glycerine

FIELD: chemistry. SUBSTANCE: invention relates to a method of producing amines and/or alkanolamines mainly containing mono- and diamine alkanols, alkyldiamines and triamines and cyclic amines by reacting glycerine with hydrogen and an aminating agent selected from the group: ammonia, methylamine and diethylamine, in the presence of a catalyst which contains a metal selected from Cu, Co, Ni, Mn, Mo, Cr, Zr, or a mixture thereof, at temperature ranging from 150°C to 300°C and pressure ranging from 20 to 300 bar, followed by separation of the end product. The process is carried out until 40-80% conversion of glycerine. The invention also relates to a method of producing amines and/or alkanolamines mainly containing mono- and diamine alkanols, alkyldiamines by reacting glycerine with hydrogen and aminating agent selected from ammonia, methylamine and diethylamine, in the presence of a catalyst which contains iridium, at temperature ranging from 150°C to 300°C and pressure ranging from 20 to 300 bar. EFFECT: method enables efficient and full utilisation of glycerine as a starting material and obtain products with high output. 11 cl, 2 tbl, 32 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 480 449 (13) C2 (51) МПК C07C 209/16 (2006.01) C07C 211/13 (2006.01) C07D 241/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010111554/04, 15.08.2008 (24) Дата начала отсчета срока действия патента: 15.08.2008 (73) Патентообладатель(и): БАСФ СЕ (DE) (43) Дата публикации заявки: 10.10.2011 Бюл. № 28 C 2 2 4 8 0 4 4 9 C 2 R U (56) Список документов, цитированных в отчете о поиске: GB 844448 А, 10.08.1960. RU 2215734 С2, 10.11.2003. SU 893940 A1, 30.12.1981. RU 2149851 С1, 27.05.2000. US 3723529 А, 27.03.1973. RU 2214434 С2, 20.10.2003. ЕР 0356046 А2, 28.02.1990. FISCHER А. ЕТ AL., "Amination of diols and polyols to acyclic amines", Catalysis today, 37, 1997, pp.167-189. (85) Дата начала рассмотрения заявки PCT на ...

팔라듐 촉매제와 그 제조 방법 및 그 이용

본 발명은 하기 NMR 스펙트라의 특성 데이터를 가지는 화합물에 관한 것으로, 상기 화합물은 팔라듐염(II)을 트리[3,5-비스(트리플루오르메틸)-페닐]포스핀과 반응시켜, 착물 염을 형성하고, 착물 염 상태의 팔라듐(II)을 팔라듐(0)으로 환원시켜 촉매 특성을 갖는 팔라듐(0) 착물을 제조하는 단계를 포함하여 제조한 것을 특징으로 하는 화합물이며, NMR 스펙트라의 특성 테이터는 하기와 같다. 1 H-NMR (300 MHz, THF-d8, d= 3.58 ppm) 8.17 (s, 12H), 7.84 (s, 24H); 13 C-NMR(75 MHz, THF-d8, d= 67.3 ppm) 138,1(C), 133.7(q, J=38.7 Hz, C),133.4(CH),126.3(CH),123.4(q, J=271.57 Hz, CF3); 31 P-NMR(300 MHz, THF-d8) 28.77; 19 F-NMR(300 MHz, THF-d8)- 62.94. 이와 같은 화합물은 대단히 안정되고, 우수한 결과를 갖는 촉매제로 이용될 수 있다.

Base-catalyzed synthesis of 1-aryl-4-(aryl ethyl)piperazines from aromatic olefins and 1-aryl piperazines

The invention relates to a method for producing a 1-aryl-4-(aryl ethyl)piperazine of formula (I) by reacting a 1-aryl piperazine of formula (II) with an aromatic olefin of formula (III) Ar'CR1=CHR2 in an inert solvent and in the presence of at least one basic catalyst, whereby in formulas (I) to (III); Ar and Ar', independent of one another, represent an aryl radical selected from the group of the condensed and non-condensed C¿6?-C22-aromatic compounds and of the condensed or non-condensed C5-C22-heteroatoms which contain at least one nitrogen, oxygen or sulfur atom in the ring; R1 and R2, independent of one another, represent a hydrogen atom, a C1-C8-alkyl radical or an aryl radical Ar.

Process for the preparation of chiral amines by homogeneously catalyzed asymmetric hydrogenation of enamines

Gegenstand der Erfindung ist ein Verfahren zur Herstellung von chiralen Aminen durch Umsetzung von elektronenreichen Enaminen in Gegenstand von Wasserstoff und eines chiralen Katalysators, umfassend mindestens einen Metall-Ligand-Komplex, der mindestens ein Metallatom ausgewählt aus der 8. Nebengruppe und ein oder mehrere mono- oder bidentate phosphorhaltige Liganden der allgemeinen Formeln (III) oder (IV) enthält, DOLLAR A (R·6·Y·1·)(R·7·Y·1·)P·1·X·1·ZX·2·P·2·(Y·2·R·8·)(Y·2·R·9·) (III) DOLLAR A (R·6·Y·1·)(R·7·Y·1·)R·8·Y·1·)P (IV) The invention relates to a process for the preparation of chiral amines by reacting electron-rich enamines with hydrogen and a chiral catalyst comprising at least one metal-ligand complex which has at least one metal atom selected from the 8th subgroup and one or more mono- or contains bidentate phosphorus-containing ligands of the general formulas (III) or (IV), DOLLAR A (R · 6 · Y · 1 ·) (R · 7 · Y · 1 ·) P · 1 · X · 1 · ZX · 2 · P · 2 · (Y · 2 · R · 8 ·) (Y · 2 · R · 9 ·) (III) DOLLAR A (R · 6 · Y · 1 ·) (R · 7 · Y · 1 ·) R · 8 · Y · 1 ·) P (IV)

一种无卤阻燃剂的制备方法及其阻燃聚烯烃组合物

本发明公开了一种无卤阻燃剂的制备方法及其阻燃聚烯烃组合物，属于阻燃剂制备领域。其中，二磷酸哌嗪的制备方法为使按比例的磷酸和哌嗪反应后，通过喷雾干燥处理制备得到二磷酸哌嗪；焦磷酸哌嗪的制备方法为结合上述二磷酸哌嗪的制备方法，将得到的二磷酸哌嗪在隋性气氛或真空条件下进行脱水缩合反应后得到。本发明还提供了一种阻燃聚烯烃组合物，该组合物包括100质量份的聚烯烃树脂、10~100质量份所述方法制备的焦磷酸哌嗪等。所述制备方法制备二磷酸哌嗪的收率>95%，焦磷酸哌嗪具有>90的以W值表示的白度。所述阻燃聚烯烃组合物具有优良的阻燃性能，焦磷酸哌嗪的添加量少，且具有优异的着色性能，具有极佳的工业应用前景。

一种高度稳定铅基有机-无机杂化钙钛矿纳米片制备方法

本发明提供了一种铅基有机‑无机杂化钙钛矿纳米片的制备方法，是通过两步法制备得到，包括以下步骤：1，将过饱和的卤化铅水溶液滴加到基底上制备卤化铅基底；2，加热有机前驱体至气相状态，与卤化铅基底充分接触并反应，得到铅基有机‑无机杂化钙钛矿纳米片。其中在气相法中，在有机前驱体中加入了疏水改性哌嗪，对卤化铅进行了处理，所得钙钛矿纳米片的浸润角增长明显，说明其抗水能力得到了提升。老化试验证明了所得钙钛矿在高温和高湿环境下能保持长时间稳定，将其制备为太阳能电池，能有不错的光电效率。本发明制备方法提供的铅基有机‑无机杂化钙钛矿纳米片综合性能优异，能同时兼具良好的光电效率和稳定性，有很好的市场推广前景。

Hydrocarbyl amines for fuel detergents

Lubricating oil additives

HYDROCARBON POLYAMINES ARE PROVIDED HAVING A LONG, SUBSTANTIALLY ALIPHATIC, OIL SOLUBILIZING HYDROCARBON CHAIN BONDED TO A DI- OR HIGHER POLYAMINE WHICH FIND USE AS DETERGENTS AND DISPERSANTS IN BOTH LUBRICATING OILS AND IN FUELS. THE HYDROCARBON GROUP IS NORMALLY BRANCHED AND DERIVED FROM NATURAL SOURCES OR POLYOLEFINS.

Process for producing heterocylic aromatic amine or arylamine

A heterocyclic aromatic halide or an aryl halide is reacted with an amine compound in the presence of a base to give a heterocyclic aromatic amine or an arylamine, respectively. In this reaction, a catalyst comprising a palladium compound and a tertiary phosphine is used for the preparation of a heterocyclic aromatic amine, and a catalyst comprising a palladium compound and a trialkylphosphine is used for the preparation of an arylamine.

Ligands for metals and metal-catalyzed processes

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

离子液体及柔粘性结晶

本发明提供一种离子液体或柔粘性结晶，其为由阴离子和阳离子构成的离子液体或柔粘性结晶，其中，阴离子含有[C(SO 2 F) 3 ] ‑ ，阳离子含有选自由1‑乙基‑3‑甲基咪唑鎓([EMI] + )、N,N‑二乙基‑N‑甲基‑(2‑甲氧基乙基)铵([DEME] + )、N‑甲基‑N‑丙基吡咯烷鎓([Py 13 ] + )、N‑甲基‑N‑丙基哌啶鎓([PP 13 ] + )、四甲基铵([N 1111 ] + )、四乙基铵([N 2222 ] + )、三甲基己基铵([N 6111 ] + )、三乙基己基铵([N 6222 ] + )、N‑甲基‑N‑乙基吡咯烷鎓([Py 12 ] + )、1‑丁基‑3‑甲基咪唑鎓([C 4 mim] + )及1‑己基‑3‑甲基咪唑鎓([C 6 mim] + )构成的组中的至少1种。

Substituted aminomethylphosphines, compositions and coordination complexes of same, their synthesis and processes using same

Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.