NOVEL PHENAZINE DERIVATIVES AND THEIR USES

The present invention is directed to novel compounds of formula I 2. The compound according to and pharmaceutically acceptable salts and solvates thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each H.11. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt or solvate thereof and at least one pharmaceutically acceptable carrier claim 1 , diluent claim 1 , excipient and/or adjuvant.12. Medicament comprising a compound according to or a pharmaceutically acceptable salt or solvate thereof.1316-. (canceled)17. A method of treating cancer comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.18. A method of treating an angiogenic disorder comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.19. A method of treating an inflammatory claim 1 , immune or infectious disease comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.20. A method for birth control claim 1 , comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof. The present invention relates to novel phenazine derivatives including their pharmaceutically acceptable salts and solvates, which are useful as anti-angiogenic and/or anti-tumor agents, in particular under hypoxic conditions.Angiogenesis is a highly regulated process, whereby new blood vessels form from preexisting ones (Folkman J. Nat. Rev. Drug Discov. 2007; 6: 273-86). In adult mammals, physiologic angiogenesis is largely limited to the ovaries, uterus, and placenta, with the turnover rate of vascular endothelial ...

SINGLETON INHIBITORS OF SUMOYLATION ENZYMES AND METHODS FOR THEIR USE

According to the embodiments described herein, a SUMOylation inhibitor compound comprising a singleton scaffold is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a singleton SUMOylation inhibitor compound. In some embodiments, the method for treating a cancer may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition. 11. The method of claim 6 , wherein the SUMOylation enzyme is SUMO E1 or SUMO E2.12. The method of claim 6 , wherein the cell is part of an in vivo population of cells in a subject.13. The method of claim 12 , wherein the population of cells is a tumor claim 12 , a population of virally infected cells claim 12 , a population of cells associated with heart disease claim 12 , a population of cells associated with a degenerative disease claim 12 , or a population of cells associated with a genetic disease.14. The method of claim 6 , wherein the cell is part of a population of cells grown in culture.15. The method of claim 14 , wherein the cell is part of a primary cell line claim 14 , a secondary cell line or an immortal cell line.16. The method of claim 15 , wherein the cell line is derived from a tumor claim 15 , a degenerative disease claim 15 , a genetic disease or a cardiovascular disease.18. The method of claim 17 , wherein the disease is a cancer claim 17 ...

Method for Preparing Curable Bicyclic Compound Derived from Biomass

The present invention relates to a curable bicyclic compound derived from biomass, solvent-free curable composition and a method for preparing thereof. The curable compound derived from biomass according to the invention comprises a bicycle structure, to which one of two epoxide functional groups are bonded. 110-. (canceled)11. A method for preparing a curable bicyclic compound derived from biomass , the method comprising:a step of preparing a starting material by preparing furan from hemicellulose extracted from biomass, maleic anhydride from cellulose extracted from biomass, or methyl acrylate from glycerol generated from biomass;a step of preparing an intermediate compound comprising bicycle and an alcohol functional group by reacting at least two of the starting materials; anda step of preparing a curable bicyclic compound comprising bicycle and an epoxide functional group by reacting the intermediate compound and epichlorohydrin.121. The method according to claim , wherein the step of preparing an intermediate compound involves reducing the intermediate compound by hydrogenation.131. The method according to claim , wherein the step of preparing a curable bicyclic compound involves reacting a mixture comprising the intermediate compound and the epichlorohydrin using PTC (Phase Transfer Catalyst) as a catalyst in a bi-phasic solvent system where a sodium hydroxide aqueous solution is added.141. The method according to claim , wherein the step of preparing an intermediate compound prepares an intermediate compound comprising bicycle and two alcohol functional groups by reacting the furan and the maleic anhydride through Diels-Alder reaction and consecutive reduction , and the step of preparing a curable bicyclic compound prepares the curable bicyclic compound comprising bicyclic and two epoxide functional groups by reacting the intermediate compound and the epichlorohydrin.15. The method according to claim 14 , wherein the step of preparing the intermediate ...

LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY DEVICE

A liquid crystal compound of formula (I): 2. The liquid crystal compound according to claim 1 , wherein A claim 1 , A claim 1 , and Aare each independently halogen-substituted or unsubstituted 1 claim 1 ,4-phenylene.3. The liquid crystal compound according to claim 2 , wherein A claim 2 , A claim 2 , and Aare each independently 1 claim 2 ,4-phenylene claim 2 , 2-fluoro-1 claim 2 ,4-phenylene claim 2 , 3-fluoro-1 claim 2 ,4-phenylene claim 2 , 2 claim 2 ,3-difluoro-1 claim 2 ,4-phenylene claim 2 , or 3 claim 2 ,5-difluoro-1 claim 2 ,4-phenylene.4. The liquid crystal compound according to claim 1 , wherein Ris a halogen atom claim 1 , —CN claim 1 , —CF claim 1 , —OCF claim 1 , —OCH═CF claim 1 , —OCFCF═CF claim 1 , a C1-C10 alkyl group or a C1-C10 alkoxyl group.5. The liquid crystal compound according to claim 1 , wherein Ris a hydrogen atom claim 1 , a C1-C5 alkyl group or a halogen-substituted C1-C5 alkyl group.6. The liquid crystal compound according to claim 1 , wherein Z claim 1 , Z claim 1 , and Zare each independently a single bond or —CFO—.7. The liquid crystal compound according to claim 1 , wherein: A claim 1 , A claim 1 , and Aare each independently 1 claim 1 ,4-phenylene claim 1 , 2-fluoro-1 claim 1 ,4-phenylene claim 1 , 3-fluoro-1 claim 1 ,4-phenylene claim 1 , 2 claim 1 ,3-difluoro-1 claim 1 ,4-phenylene claim 1 , or 3 claim 1 ,5-difluoro-1 claim 1 ,4-phenylene; Z claim 1 , Z claim 1 , and Zare each independently a single bond or —CFO—; n=0; and m=0 or 1.8. A liquid crystal composition comprises the liquid crystal compound according to .10. The liquid crystal composition according to claim 9 , wherein Ris a hydrogen atom claim 9 , a C1-C10 alkyl group claim 9 , and Ris a halogen atom claim 9 , —CN claim 9 , a C1-C10 alkyl group claim 9 , a C2-C10 alkenyl group claim 9 , —OCHCF claim 9 , —CF claim 9 , or —OCF.11. A liquid crystal display device comprising a liquid crystal compound according to . This application claims the priority of Taiwan application ...

A PROCESS FOR PREPARING AN OPTICALLY ACTIVE CINEOLE DERIVATIVE

The present invention relates to a process for preparing optically active 1,4-cineole derivatives by enzymatic resolution and enantiomerically pure optically active 1,4-cineole derivatives of purity greater than 99.9% that have been prepared by this process. The present invention further relates to a process for preparing 7-oxabicyclo[2.2.1]heptane derivatives from the enantiomerically pure optically active 1,4-cineole derivatives. 115-. (canceled)17. The process of claim 16 , further comprising the steps of(iii) subjecting the mixture of step (ii) to basic saponification to obtain a mixture containing the first enantiomer of the compounds of formula (I) in unacylated form; and(iv) isolating the first enantiomer of the compounds of formula (I) in unacylated form from the mixture of step (iii) to obtain an optically active compound of formula (II-R) or an optically active compound of formula (II-S).18. The process of claim 16 , further comprising the steps ofv) providing a suspension comprising the optically active compound of formula (II-R) or formula (II-S) as obtained in step (iv) in at least one non-polar solvent;vi) stirring the suspension obtained in step (v) at temperature in the range of ≥10° C. to reflux temperature of the non-polar solvent; andvii) isolating the crystals of the optically active enantiomer of formula (II-R) or formula (II-S) obtained in step (vi).19. The process of claim 18 , further comprising adding seed crystals of the desired enantiomer of formula (I-R) or formula (I-S) in step (vi).20. The process of claim 16 , wherein in the mixture in step (i)(a) the first enantiomer of the compounds of formula (II) in acylated form is the optically active compound of formula (II-S) and the second enantiomer of the compounds of formula (II) in unacylated form is the optically active compound of formula (II-R); or (b) the first enantiomer of the compounds of formula (II) in acylated form is the optically active compound of formula (II-R) and the second ...

CHROMENE COMPOUND

A novel photochromic compound which develops a color of a neutral tint (double peak characteristic) and has high color optical density, high fading speed and excellent durability. 2. A photochromic curable composition which comprises the chromene compound of and polymerizable monomers.3. A photochromic optical article having a polymer molded body containing the above chromene compound of dispersed therein as a constituent member.4. An optical article having an optical substrate at least one surface or all of which is covered with a polymer film containing the chromene compound of dispersed therein as a constituent member. The present invention relates to a novel chromene compound which is useful as a photochromic compound for photochromic spectacle lenses.Photochromism is the reversible function of a certain compound that it changes its color swiftly upon exposure to light including ultraviolet light such as sunlight or light from a mercury lamp and returns to its original color when it is put in the dark by stopping its exposure to light. A compound having this property is called “photochromic compound” and used as a material for photochromic plastic lenses.For the photochromic compound used for this purpose, the following properties are required: (I) the degree of coloration at a visible light range before ultraviolet light is applied (to be referred to as “initial coloration” hereinafter) should be low, (II) the degree of coloration upon exposure to ultraviolet light (to be referred to as “color optical density” hereinafter) should be high, (III) the speed from the time when the application of ultraviolet light is started to the time when the color optical density reaches saturation (to be referred to as “color development sensitivity” hereinafter) should be high; (IV) the speed from the stoppage of the application of ultraviolet light to the time when the compound returns to its original state (to be referred to as “fading speed” hereinafter) should be high, (V) ...

Process for preparing 2-exo-(2-methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane

This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-iso-propyl-7-oxabicyclo[2.2.1]heptane of the formula (I) any of its individual enantiomers or any non-racemic mixture thereof, comprising the step of reacting (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (II) any of its individual enantiomers or any non-racemic mixture thereof with a 2-Methylbenzyl compound of the formula (III) wherein X is a leaving group, in the presence of at least one base, at least one catalyst selected from rubidium salts, cesium salts and any combination thereof and at least one inert organic solvent S1.

PROCESS FOR PREPARING BICYCLIC ENOLETHER

Described herein is a process for preparing a compound of formula (I) 2. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.3. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.4. The process according to according to claim 1 , characterized in that Rrepresents a 1 claim 1 ,2-propanediyl group or 1 claim 1 ,2-ethanediyl group.5. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.6. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.7. The process according to claim 1 , characterized in that Rrepresents a 1 claim 1 ,8-octanediyl group.8. The process according to claim 1 , characterized in that compound of formula (I) is selected from the group consisting claim 1 , of 12-oxabicyclo[6.3.1]dodec-8-ene claim 1 , 10-methyl-12-oxabicyclo[6.3.1]dodec-8-ene claim 1 , 13-oxabicyclo[7.3.1]tridec-9-ene claim 1 , 11-methyl-13-oxabicyclo[8.3.1]tridec-9-ene claim 1 , 14-oxabicyclo[8.3.1]tetradec-10-ene claim 1 , 12-methyl-14-oxabicyclo[8.3.1]tetradec-10-ene claim 1 , 15-oxabicyclo[9.3.1]pentadec-11-ene claim 1 , 13-methyl-15-oxabicyclo[9.3.1]pentadec-11-ene claim 1 , 16-oxabicyclo[10.3.1]hexadec-12-cue claim 1 , 14-methyl-16-oxabicyclo[10.3.1]hexadec-12-ene claim 1 , 17-oxabicyclo[11.3.1]heptadec-13-ene and 15-methyl-17-oxabicyclo[11.3.1]heptadec-1.3-ene.9. The process according to claim 1 , characterized in that compound of formula (II) is selected from the group consisting of cycloundecane-1 claim 1 ,5-dione claim 1 , 3-methylcycloundecane-1 claim 1 ,5-dione claim 1 , cyclododecane-1 claim 1 ,5-di one claim 1 , 3-methylcyclododecane-1 claim 1 ,5-dione claim 1 , cyclotridecane-1 claim 1 ,5-dione claim 1 , methylcyclotridecane-1 claim 1 ,5-dione claim 1 , cyclotetradecane-1.5-dione claim 1 , 3-methylcyclotetradecane-1 claim 1 ,5-dione claim 1 , ...

OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES, THEIR PREPARATION AND USE

This invention provides compounds having the structure 153-. (canceled)55. (canceled)57. The method of claim 54 , wherein bond α is present.58. The method of claim 54 , wherein bond α is absent.64. The method of claim 54 , wherein Rand Rtogether are ═O.65. The method of claim 54 , wherein Rand Rare each H. The present application is a divisional of U.S. Ser. No. 12/069,147, filed Feb. 6, 2008, which claims the benefit of U.S. Provisional Application 61/011,323, filed Jan. 15, 2008, U.S. Provisional Application No. 60/964,904, filed Aug. 14, 2007 and U.S. Provisional Application No. 60/899,903, filed Feb. 6, 2007, the contents of each of which are hereby incorporated by reference.Throughout this application, certain publications are referenced. Full citations for these publications may be found immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by reference into this application in order to describe more fully the state-of-the art to which this invention relates.Retinoids, metabolites of vitamin A, have been examined therapeutically against a variety of tumors, including gliomas. (Yung et al. (1996)) Nuclear receptor co-repressor (N-CoR) is closely associated with the retinoid receptor and is released upon ligand binding to the receptor. (Bastien et al. (2004)) By preventing the action of protein phosphatase-1 and protein phosphatase-2A, anti-phosphatases increase the phosphorylated form of N-CoR and promotes its subsequent cytoplasmic translocation. (Hermanson et al. (2002))The phosphatase inhibitor, Cantharidin, has anti-tumor activity against human cancers of the liver (hepatomas) and of the upper gastrointestinal tract but is toxic to the urinary tract (Wang, 1989).The publication of a report that cantharidin acts as a protein phosphatase inhibitor prompted a more general interest in compounds with this type of chemical structure (Li and Casida, 1992). Previously, it had been found that the simpler ...

COMPOUND AND ORGANIC LIGHT-EMISSION DEVICE

The present invention provides a novel compound of an amine derivative including a spiro compound. The novel compound has excellent hole transport characteristics. Thus, when the novel compound is applied to a hole transport layer, an auxiliary hole transport layer and an electron blocking layer of an organic light-emitting device, the device realizes low driving voltage, high efficiency, high thermal stability and long life-span. Further, when the novel compound is applied as a blue light-emitting material, the device realizes a low driving voltage and high efficiency. 4. An organic light-emission device comprising:an anode,a cathode, and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one organic material layer therebetween, wherein the organic material layer comprises a compound of .'}5. The organic light-emission device of claim 4 , wherein the organic material layer includes at least one of a hole transport layer claim 4 , an auxiliary hole transport layer and an electron blocking layer claim 4 , wherein the at least one of the hole transport layer claim 4 , the auxiliary hole transport layer and the electron blocking layer comprises the compound represented by Chemical Formula 1.6. The organic light-emission device of claim 5 , wherein the hole transport layer comprises the compound represented by Chemical Formula 1.7. The organic light-emission device of claim 5 , wherein the auxiliary hole transport layer comprises the compound represented by Chemical Formula 1.8. The organic light-emission device of claim 5 , wherein the electron blocking layer comprises the compound represented by Chemical Formula 1.9. The organic light-emission device of claim 4 , wherein the organic material layer comprises a blue light-emission layer comprising the compound represented by Chemical Formula 1 as a blue light-emission material.10. The organic light-emission device of claim 4 , wherein the organic material layer includes at least one of an electron transport ...

PROCESS FOR PREPARING 2-EXO-(2-METHYLBENZYLOXY)-1-METHYL-4-ISOPROPYL-7-OXABICYCLO[2.2.1]HEPTANE

This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-iso-propyl-7-oxabicyclo[2.2.1]heptane of the formula (I), (I) any one of its individual enantiomers or any non-racemic mixture thereof comprising the steps of (a) deprotonating (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (II), (II) any one of its individual enantiomers or any non-racemic mixture thereof in the presence of at least one base of the formula [Mm+]n [An-]m (III) wherein Mm+ represents a m-valent metal cation wherein m is an integer of 1 or 2, and An_ represents a n-valent anion wherein n is an integer of 1 or 2, said base being capable of forming a solvent S1 selected from water, a C1-C4 alkyl alcohol or any combination thereof under the reaction conditions, to form a metal alkoxide or metal alkoxide solvate of the formula (IV), (IV) any one of its individual enantiomers or any non-racemic mixture thereof wherein M, m and the solvent S1 have the same meaning as defined for the base of formula (III), and x denotes a number from 0 to 10, and (b) reacting the metal alkoxide or metal alkoxide solvate of the formula (IV), any of its individual enantiomers or any non-racemic mixture thereof with a 2-Methylbenzyl compound of the formula (V), (V) wherein X is a leaving group, wherein the steps (a) and (b) are conducted in the presence of at least one inert organic solvent S2 and comprise a further step of (c) simultaneously removing the solvent S1 from the reaction mixture. 118-. (canceled)20: The process according to wherein claim 19 , in further step (c) claim 19 , the solvent S1 is removed from the reaction mixture by azeotropic distillation.21: The process according to wherein the further step (c) comprises the steps of(c.1) simultaneously removing the solvent S1 from the reaction mixture as an azeotrope formed by the inert organic solvent S2 and the solvent S1, and(c.2) adding the inert organic solvent S2 or a mixture comprising ...

COMMERCIALLY VIABLE SYNTHESIS OF CANTHARIDIN AND BIOACTIVE CANTHARIDIN DERIVATIVES

The present disclosure provides methods for synthesizing cantharidin and cantharidin derivatives. 1. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative at an exo-to-endo ratio of at least 6:1.28-. (canceled)9. The method of claim 1 , wherein said reacting is conducted at a pressure less than about 100 atm.1012-. (canceled)14. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative claim 1 , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative claim 1 , wherein said reacting is conducted (i) in the absence of diethyl ether claim 1 , (ii) in the absence of a lithium or magnesium salt claim 1 , and (iii) at a pressure less than about 980 atmospheres (atm).1521-. (canceled)22. The method of claim 14 , wherein said reacting is conducted with the aid of a catalyst.2324-. (canceled)25. The method of claim 22 , wherein said catalyst comprises bis(cyclopentadienyl)zirconium(IV) bis(trifluoromethanesulfonate)tetrahydrofuran complex.26. The method of claim 22 , wherein said catalyst comprises aluminum chloride.2729-. (canceled)30. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative claim 22 , (ii) less than 0.1% diethyl ether and (iii) less than 0.1% lithium salt claim 22 , wherein said cantharidin or cantharidin derivative is at an exo-to-endo ratio of at least 6:1.3136-. (canceled)37. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative and (ii) a Lewis catalyst comprising one or more Lewis metals selected from the group consisting of Li (I) claim 22 , Mg (II) claim 22 , B (III) claim 22 , Al (III) claim 22 , Ti (IV) claim 22 , Zr ...

COMPOUNDS AND COMPOSITIONS FOR INDUCING CHONDROGENESIS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating joint damage or injury in a mammal, for inducing hyaline cartilage production or for inducing differentiation of chondrogenic progenitor cells into mature chondrocytes. 123-. (canceled)26. The compound of claim 25 , or a pharmaceutically acceptable salt claim 25 , or stereoisomer thereof claim 25 , wherein said compound is of Formula (1A) claim 25 , Formula (1G) claim 25 , Formula (1L) claim 25 , Formula (2A) claim 25 , Formula (2G) or Formula (2L).27. The compound of claim 24 , wherein one of Rand Ris hydrogen and the other is hydroxyl; and Rand Rare hydrogen.28. The compound of claim 24 , wherein one of Rand Rand one of Rand Rtogether with the carbon ring atoms form a cyclopropyl fused to the bicyclic ring.29. The compound of claim 24 , wherein Ris phenyl claim 24 , pyridyl claim 24 , pyrazolyl claim 24 , thiazolyl or piperidinyl claim 24 , each of which is unsubstituted or substituted by 1 to 2 substituents independently selected from halo claim 24 , Calkyl claim 24 , halo-substituted Calkyl claim 24 , Calkoxy claim 24 , halo-substituted Calkoxy claim 24 , cyano claim 24 , Calkylsulfonyl claim 24 , phenyl unsubstituted or substituted by halo.30. The compound of claim 29 , wherein Ris selected from:phenyl substituted by 3,4-dichloro; 2-trifluoromethyl; 3-trifluoromethyl; 3-cyano-4-chloro; 2-cyano-4-chloro; 3-fluoro-4-chloro; 3-trifluoromethoxy; 3-fluoro-4-trifluoromethoxy; or 3-chloro-4-(2-fluorophenyl);pyridin-4-yl substituted by 6-methoxy or 2-trifluoromethyl;pyridin-3-yl substituted by 5,6-dichloro; 6-methoxy; 5-chloro-6-methyl or 5-trifluoromethyl-6-methyl;pyridin-2-yl substituted by 4,5-dichloro; ...

PARTHENOLIDE DERIVATIVES AND THEIR MODULATION OF PROCESSES CONTROLLED BY REGULATED TRANSLATION

The present invention provides parthenolide derivatives. In particular, the present invention provides parthenolide derivatives that modulate processes controlled by regulated mRNA translation and have anticancer activity. 2. The method of claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , substituted alkyl claim 1 , alkenyl claim 1 , substituted alkenyl claim 1 , alkynyl claim 1 , substituted alkynyl claim 1 , amine claim 1 , carbocyclic claim 1 , substituted carbocyclic claim 1 , heterocyclic claim 1 , or substituted heterocyclic; each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris hydrogen; Ris alkyl claim 1 , alkyl alcohol claim 1 , ether claim 1 , or ester; and Ris alkyl.3. (canceled)4. The method of claim 1 , wherein regulated mRNA translation is regulated by a sequence-specific mRNA binding protein chosen from a Pumilio claim 1 , a Musashi claim 1 , or a cytoplasmic polyadenylation element binding (CPEB) protein.5. The method of claim 1 , wherein the process controlled by regulated mRNA translation is cell cycle progression claim 1 , cell growth control claim 1 , cell division control claim 1 , cell survival control claim 1 , or signal transduction.6. The method of claim 1 , wherein the cell is disposed in a subject.8. The compound of claim 7 , wherein Ris alkyl claim 7 , substituted alkyl claim 7 , alkenyl claim 7 , substituted alkenyl claim 7 , alkynyl claim 7 , substituted alkynyl claim 7 , amine claim 7 , carbocyclic claim 7 , substituted carbocyclic claim 7 , heterocyclic claim 7 , or substituted heterocyclic; each of R claim 7 , R claim 7 , R claim 7 , R claim 7 , and Ris hydrogen; Ris hydrogen claim 7 , alkyl claim 7 , substituted alkyl claim 7 , alkenyl claim 7 , substituted alkenyl claim 7 , alkynyl claim 7 , substituted alkynyl claim 7 , aryl claim 7 , or substituted aryl; and Ris alkyl.9. The compound of claim 7 , wherein the optional single bond is present and Ris —NRR claim 7 , in which Ris hydrogen and Ris alkyl claim 7 , ...

ANALOGS OF ADAMANTYLUREAS AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS

N-(2-oxaadamantan-1-yl)ureas of formula I, where R3 is H, C-Calkyl, cyclohexyl or phenyl; R is —[CH]—Y; n is 0-15; in —[CH]— 0-n/3 of the methylene groups are optionally replaced by non adjacent oxygen atoms; and Y is a 3- or 4-substituted phenyl, a 3- or 4-substituted cyclohexyl, a N-substituted piperidin-4-yl, a N-substituted piperidin-3-yl, a di- or tri-fluorosubstituted phenyl, 4-chloro-3-trifluoromethylphenyl, 3-chloro-4-trifluoromethylphenyl, 4-fluoro-3-trifluoromethylphenyl, or 3-fluoro-4-trifluoromethylphenyl; have epoxide hydrolase (sEH) inhibitory activities similar to those of their N-(adamantan-1-yl)urea analogs. Thus, compounds I are useful as API for the treatment of sEH mediated diseases. Besides, in general, compounds I have higher water solubilities and lower melting points, what make them more promising from the point of view of pharmacokinetics and formulation. 3. The compound according to claim 2 , wherein Y is a radical selected from the group consisting of:di- and a tri-fluorosubstituted phenyl radicals;4-chloro-3-trifluoromethylphenyl;3-chloro-4-trifluoromethylphenyl;4-fluoro-3-trifluoromethylphenyl;3-fluoro-4-trifluoromethylphenyl; and{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'claim-text': [{'sub': 3', '3, 'H, F, Cl, CF, OCF, OH, CN, COOH;'}, {'sub': 2', '2, 'phenyl, phenoxy, mono-substituted phenyl and mono-substituted phenoxy, wherein the substituent is COOH, Cl or HNSO;'}, {'sub': 1', '15', '1', '15', '1', '15, 'claim-text': {'sub': 1', '15', '1', '15', '1', '15', '2', '1', '15', '2', '1', '15', '2, '(C-Clinear alkyl)NHCO, (C-Clinear alkyl)CONH, (C-Clinear alkyl)SO(C-Clinear alkyl)NHSO, (C-Clinear alkyl)SONH;'}, '(C-Clinear alkyl)O, (C-Clinear alkyl)CO, (C-Clinear alkyl)OCO,'}, '(5/6-membered-N/O-heterocyclyl)O, (5/6-membered-N/O-heterocyclyl)CO, (5/6-membered-N/O-heterocyclyl)OCO, (5/6-membered-N/O-heterocyclyl)-NHCO, (5/6-membered-N/O-heterocyclyl)CONH;', {'sub': 2', '2', '2, '(5/6-membered-N/O-heterocyclyl)SO, (5/6-membered-N/O- ...

SANDWICH ASSAY DESIGN FOR SMALL MOLECULES

Methods are disclosed of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2,000. The method comprises preparing a first antibody that binds to the small molecule, and preparing a second antibody that binds to the small molecule at a portion of the small molecule other than a portion to which the first antibody binds. The second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule. The antibodies may be employed in sandwich assays for the small molecule. 1(a) preparing a first monoclonal antibody that binds specifically to a binding domain extending approximately from ring atom 15 to ring atom 21 and includes a triene moiety from ring atom 17 to ring atom 22 of sirolimus, wherein the first antibody is prepared from an immunogen that comprises sirolimus, wherein sirolimus is linked at carbon atom 26 or 32 through an oxime functionality to an immunogenic carrier for eliciting antibodies; and(b) preparing a second monoclonal antibody that binds specifically to sirolimus in a portion other than the domain to which the first antibody binds, wherein said second antibody binds a binding domain extending approximately from the methyl group on atom 11 to the methoxy group on atom 39 or from the methyl group on ring atom 25 to atom 41, wherein the second monoclonal antibody is prepared from an immunogen that comprises sirolimus that is modified in the triene area extending approximately from ring atom 15 to ring atom 21 and including a triene moiety from ring atom 17 to ring atom 22, to which the first monoclonal antibody binds, wherein sirolimus is combined with a cyclic reagent IV under conditions for carrying out a Diels-Aider-reaction to produce a modified sirolimus of formula IA and IIB and the modified sirolimus is linked to an immunogenic carrier at ring atom 26 or ring atom 32 for eliciting antibodies;wherein IIA, IIB, and reagent IV are compounds of the formula ...

PIMARANE DITERPENES FROM ANISOCHILUS VERTICILLATUS

This invention discloses diterpenes class of novel compounds of general formula I from a novel source. More particularly the invention relates to extracts/fractions containing pimarane diterpenes from (Lamiaceae), useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further relates to extracts, fractions standardized to diterpenes class of novel compounds useful for the treatment of cancers. 3Anisochilus verticillatus.. The compounds as claimed in claim 1 , wherein said compound is isolated from4. The compound as claimed in are useful for prevention claim 1 , treatment claim 1 , inhibition or controlling growth and proliferation of cancer/tubercular activity in mammals.5. The compounds as claimed in are useful for treating or controlling proliferation of tuberculosis in a mammal.6. The compounds as claimed in claim 1 , wherein % inhibition on Thp-1 cell line of compound 3 is 57.23 at 100 μg/ml.7M. tuberculosis. The compounds of general formula I as claimed in claim 1 , wherein ICvalue of compounds of general formula I against is in the range of 12.5 to 42.92 μg/ml.8. A process for the extraction of compounds of general formula I as claimed in claim 1 , wherein the process comprises the steps of:{'i': 'A. verticillatus', 'i). pulverizing aerial parts of followed by extraction with acetone at room temperature in the range of 25 to 30° C., filtering acetone solubles and concentrating under reduced pressure in the range of 50-100 mm Hg to obtain a greenish acetone extract,'}ii) separating the extract as obtained in step i) by using column chromatography (CC) with increasing polarity of the polar solvent with gradient of acetone from 5% to 50% in pet ether to obtain 18 fractions (AV1-AV18).iii) subjecting fraction AV3 of step ii) to CC with gradient of acetonitrile from 0.5% to 3% in chloroform to collect 8 fractions (AV3a-h),iv) subjecting fraction AV4 of step ii) CC using gradient of ...

Induction of highly specific antibodies to a hapten but not to a carrier peptide by immunization

In this application Is described a composition and method for Inducing In a subject anti-hapten antibodies without Inducing antibodies to the carrier protein. Kits for designing and making compositions with desired haptens are also described. In this application Is disclosed a synthetic liposome composition comprising liposomes (L) containing monophosphoryl lipid A (MPLA) [L(MPLA)] and an immunoconjugate comprising a carrier and a hapten. In one embodiment, the carrier is a 23 amino acid hydrophobic membrane proximal external region peptide (MPER) derived from the gp41 transmembrane protein of HIV-1 that spontaneously associates with the outer surface of bilayers of liposomes containing MPLA during liposome formation. 1. A hapten with a chemical formula chosen from the following:(i) N-((4R,4aR,7R,7aR,12bS)-9-hydroxy-3-methyl-2,3,4,4a,7,7a-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-mercaptopropanamide;(ii) (4R,4aR,7S,7aR,12bS)-9-(3-mercaptopropanamido)-3-methyl-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl acetate;(iii) N,N′-((4R,4aR,7S,7aR,12bs)-3-(4-(3-mercaptopropanamido)butyl)-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diyl)diacetamide;(iv) N-((4R,4aR,7S,7aR,12bS)-7-acetamido-3-methyl-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl)-3-mercaptopropanamide;(v) 3-mercapto-N-((4R,4aR,7R,7aS,12bS)-3-methyl-7-(2-oxopropyl)-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl)propanamide; and(vi) N-(4-((4R,4aR,7R,7aS,12bS)-7,9-bis(2-oxopropyl)-4,4a,5,6,7,7a-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3(2H)-yl)butyl)-3-mercaptopropanamide.2. An immunoconjugate wherein a hapten of is covalently linked to a carrier moeity.3. An immunoconjugate comprising a hapten with a structural formula:N-((4R,4aS,7R,7aR,12bS)-4a,9-dihydroxy-3-methyl-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-mercaptopropanamide.4 ...

INTERMEDIATES TO PREPARE HERBICIDAL PYRIMIDONE DERIVATIVES

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, 117.-. (canceled) This invention relates to certain bis-nitrogen heterocycles, their salts and compositions, and methods of their use for controlling undesirable vegetation. This invention also relates to certain intermediates and a method useful for preparing these bis-nitrogen heterocycles and their salts. This invention also relates to certain bis-nitrogen oxo or sulfono heterocycles, their salts and compositions, and methods of their use for controlling undesirable vegetation.The control of undesired vegetation is extremely important in achieving high crop efficiency. Achievement of selective control of the growth of weeds especially in such useful crops as rice, soybean, sugar beet, maize, potato, wheat, barley, tomato and plantation crops, among others, is very desirable. Unchecked weed growth in such useful crops can cause significant reduction in productivity and thereby result in increased costs to the consumer. The control of undesired vegetation in noncrop areas is also important. Many products are commercially available for these purposes, but the need continues for new compounds that are more effective, less costly, less toxic, environmentally safer or have different sites of action.International patent application publication WO 2007/088876 discloses pyridone compounds of Formula iwherein inter alia Ris C-Calkyl; Rand Rare each independently hydrogen, cyano, or nitro; and A is a A-1 through A-5 as defined therein as herbicides.The bis-nitrogen containing oxo and sulfono heterocycles of the present invention are not disclosed in this publication.This invention is directed to compounds of Formula 1 (including all stereoisomers), N-oxides, and salts thereof, agricultural compositions containing them and their use as herbicides:whereinMore particularly, this invention pertains to a compound of Formula 1 (including all stereoisomers), an N-oxide, or a salt ...

FATTY ACID AMIDE HYDROLASE INHIHIBITORS FOR TREATING PAIN

The present invention provides a method of treating a patient suffering from pain or other FAAH mediated conditions by administering a fatty acid amide inhibiting amount of a compound represented by the formula: wherein Ris H; Ris a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; Ris a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; X is CHCH, (CH)or O(CH), wherein n is 0 or an integer of from 1 to 4; and W is O, S, or NR, wherein Ris selected from the group consisting of H and alkyl. 2. The method of wherein W is O.3. The method of wherein Ris a radical selected from the group consisting of H claim 1 , alkyl claim 1 , haloalkyl and aryl.4. The method of wherein Ris selected from the group consisting of ethyl claim 2 , methyl claim 2 , 2-methylethyl claim 2 , phenyl claim 2 , trifluoromethyl and 2 claim 2 , 2 claim 2 , 2 trifluoroethyl.5. The method of wherein Ris selected from the group consisting of H claim 1 , alkyl claim 1 , alkenyl and aryl.6. The method of wherein Ris selected from the group consisting of n-alkyl and cycloalkyl-n-alkyl7. The method of wherein claim 5 , Ris (CH)CHR claim 5 , wherein n is an integer of from 4 to 9 and Ris H or cycloalkyl.8. The method of wherein Ris selected from the group consisting of cyclohexyl-n-alkyl radicals.9. The method of wherein Ris cyclohexyl-n-butyl.10. The method of wherein X is ethyl or ethenyl.11. The method of wherein said compound is selected from the group consisting of(E)-3R-[2R-[[3-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]-7-oxabicyclo[2.2.1]hept-2-yl]methyl]-4-fluoro-phenyl]-N-(ethylsulfonyl)acrylic amide,(E)-3R-[2R-[[3-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]-7-oxabicyclo[2.2.1]hept-2-yl]methyl]-4-fluoro-phenyl]-N-(methylsulfonyl)acrylic amide,(E)-3R-[2R-[[3-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]-7-oxabicyclo[2.2.1]hept-2-yl]methyl]-4-fluoro-phenyl]-N-(2,2,2-trifluoroethanesulfonyl)acrylic ...

OXANORBORNADIENE DERIVATIVES AND THEIR ANTICANCER ACTIVITIES

The present invention relates to chemical entities originated from natural sources and further synthesized for therapeutic uses. More particularly, the present invention relates to norcantharidin analogues synthesized by a transition metal-catalyzed alkynylation of oxanorbornadiene derivatives and their antitumor effects. 3. The composition of claim 1 , wherein oxanorbornadiene derivatives are first isolated from a natural source or obtained from a chemically synthesized compound claim 1 , followed by reacting said oxanorbornadiene derivatives with a chemical ligand under a transition metal-catalyzed alkynylation reaction in the presence of a solvent in order to result in said norcantharidin analogues.4. The composition of claim 3 , wherein a transition metal used in said transition metal-catalyzed alkynylation reaction is an iridium-based compound.5. The composition of claim 4 , wherein said iridium-based compound comprises Ir(I)(COD)Cl claim 4 , [Ir(I)(COD)Cl] claim 4 , Ir(I)(COD)(acac) and Ir(III)(CH)(acac).6. The composition of claim 3 , wherein said solvent comprises 1 claim 3 ,2-dichloroethane claim 3 , tetrahydrofuran claim 3 , dimethoxyethane claim 3 , toluene claim 3 , EtOAc and i-PrOH.7. The composition of claim 3 , wherein said chemical ligand is 4-Ethynylanisole.8. The composition of is administered to a subject in need thereof in order to prevent and/or treat the cancer or tumor in said subject.9. The composition of claim 8 , wherein said cancer or tumor comprises hepatoma claim 8 , breast claim 8 , oesophageal claim 8 , colorectal and lung carcinoma.11. The method of claim 10 , wherein said transition metal-catalyzed alkynylation comprising using an iridium-based catalyst.12. The method of claim 11 , wherein said iridium-based catalyst comprises Ir(I)(COD)Cl claim 11 , [Ir(I)(COD)Cl] claim 11 , Ir(I)(COD)(acac) and Ir(III)(CH)(acac).13. The method of claim 10 , wherein said chemical ligand is 4-Ethynylanisole.14. The method of claim 10 , wherein said ...

6,11-BRIDGED BIARYL MACROLIDES

The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1. A compound represented by the formula (I) or (II):as well as the pharmaceutically acceptable salts, esters and prodrugs thereof, wherein:{'sub': 3', '1', '2', '1', '2, 'claim-text': (a) hydrogen;', {'sub': 3', '3', '1', '6', '2', '6', '2', '6, '(b) —R, wherein Ris substituted or unsubstituted —C-Calkyl, —C-Calkenyl, or —C-Calkynyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N;'}, {'sub': 4', '4, 'claim-text': (i) hydrogen;', '(ii) aryl; substituted aryl; heteroaryl; substituted heteroaryl;', {'sub': '3', '(iii) —R; and'}, {'sub': 5', '5', '3', '12, '(iv) —R, wherein Ris substituted and unsubstituted —C-Ccycloalkyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N;'}], '(c) —C(O)R; wherein Ris independently selected from the group consisting of, {'sub': '4', '(d) —C(O)NHR;'}, {'sub': '4', '(e) —C(O)OR; and'}, {'sub': 2', '4, '(f) —S(O)R;'}], 'T is hydrogen, OR, halogen or NRR, wherein Rand Rare each independently selected from{'sub': 1', '2, 'alternatively, Rand Rcan be taken together with the nitrogen they are attached with to form a fused or non-fused, substituted or unsubstituted heterocyclic ring;'}{'sub': '1', 'Yis S or O;'}{'sub': 2', '3', '10', '10', '3', '2', '3, 'Yand Yare each independently selected S, N, O or CR; wherein Ris independently selected from hydrogen, hydroxy, amino, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamino, substituted or unsubstituted dialkylamino, CF, CN, NO, N, sulfonyl, acyl, aliphatic, and substituted aliphatic;'}{'sub': 1', '3', '2, 'provided that when either Yor Yis S and Yis CH or N, T is not hydrogen;'}{'sub': 1', '2', '3', '10, 'X, Xand Xare each independently selected N or CR;'}Cy is substituted or unsubstituted heterocyclic, or substituted or unsubstituted heteroaryl; (a) hydrogen;', {'sub': '3', '(b) —R;'}, {'sub': '4', ...

Asymetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities

The present invention relates to a type of norcantharidin analogues and a method to synthesis such norcantharidin analogues by transition metal-catalyzed alkynylation of 7-oxabenzonorbornadienes. The present invention also relates to the use of such norcantharidin analogues in manufacture of a medicament for the treatment of cancer tumors.

ANTIVIRAL COMPOSITION AND METHOD FOR CONTROLLING PLANT VIRUSES USING THE SAME

A method for controlling plant viruses comprising treating plant or soil with a composition for controlling plant viruses comprising Trichodermin wherein the composition has antiviral activity against plant viruses when applied to a plant or to soil. In some embodiments, the Trichodermin is isolated from a strain. 2Trichoderma albolutescens. The method of claim 1 , wherein the Trichodermin is isolated from a strain.3Trichoderma albolutescensTrichoderma albolutescenes. The method of claim 2 , wherein the strain is KUC2115 strain claim 2 , Deposit No. KACC93215P.4. The method according to claim 1 , wherein the plant virus is at least one selected from the group consisting of a tobacco mosaic virus (TMV) claim 1 , a pepper mottle virus (PepMoV) claim 1 , a cucumber mosaic virus (CMV) claim 1 , a pepper mild mottle virus (PMMoV) claim 1 , a zucchini yellow mosaic virus (ZYMV) claim 1 , a watermelon mosaic virus (WMV) claim 1 , a watermelon mosaic virus2 (WMV2) claim 1 , a potato virus Y(PVY) claim 1 , a turnip mosaic virus (TuMV) claim 1 , a melon necrotic spot carmovirus (MNSV) claim 1 , a cucumber green mottle mosaic virus (CGMMV) claim 1 , a zucchini green mottle mosaic virus (ZGMMV) claim 1 , a potato leafroll virus (PLRV) claim 1 , a lily mottle virus (LMoV) claim 1 , a lily symptomless virus (LSV) claim 1 , an odontoglossum ringspot virus (ORSV) claim 1 , a cymbidium mosaic virus (CyMV) claim 1 , a broad bean wilt virus (BBWV) claim 1 , a tomato ringspot virus (TomRSV) claim 1 , a tobacco ringspot virus (TRSV) claim 1 , a tomato spotted wilt virus (TSWV) claim 1 , a strawberry mottle virus (SMoV) and a cactus X virus (CVX).5. The method of claim 1 , wherein the composition is formulated into at least one selected from the group consisting of solutions claim 1 , granules claim 1 , powders claim 1 , emulsions claim 1 , oil solutions claim 1 , wettable powders and pastes.6Trichoderma albolutescenes. The method of claim 1 , wherein the composition comprises a ...

MODIFIED BIOTIN, MUTANT STREPTAVIDIN, AND USE THEREOF

It is an object of the present invention to provide a mutant streptavidin with a reduced affinity for natural biotin, and also to provide a modified biotin having a high affinity for the mutant streptavidin with a reduced affinity for natural biotin. According to the present invention, there is provided a reagent kit for use in treatments or diagnoses, which comprises: (a) a mutant streptavidin with a reduced affinity for natural biotin or biocytin; and a modified biotin having a high affinity for the above-described mutant streptavidin. 4. A mutant streptavidin comprising the amino acid sequence shown in any one of SEQ ID NOS: 3 to 12.5. DNA encoding the mutant streptavidin according to .6. A mutant streptavidin-molecular probe conjugate which is obtained by conjugating a molecular probe to the mutant streptavidin according to .7. A therapeutic agent or an in-vivo or in-vitro diagnostic agent claim 6 , which comprises the mutant streptavidin-molecular probe conjugate according to .8. A therapeutic claim 1 , or in-vivo or in-vitro diagnostic kit claim 1 , which comprises: (a) a mutant streptavidin-molecular probe conjugate which is obtained by conjugating a molecular probe to a mutant streptavidin comprising the amino acid sequence shown in any one of SEQ ID NOS: 3 to 12; and (b) an in-vivo or in-vitro diagnostic or therapeutic substance that has been labeled with the compound according to .9. A reagent kit for use in treatments or in-vivo or in-vitro diagnoses claim 1 , which comprises:(a) a mutant streptavidin with a reduced affinity for natural biotin or biocytin; and(b) a modified biotin having a high affinity for the above-described mutant streptavidin.10. A therapeutic claim 1 , or in-vivo or in-vitro diagnostic kit claim 1 , which comprises:(a) a conjugate of a mutant streptavidin with a reduced affinity for natural biotin or biocytin and a molecular probe; and(b) an in-vivo or in-vitro diagnostic or therapeutic substance that has been labeled with a modified ...

DIELS-ALDER REACTIONS CATALYZED BY LEWIS ACID CONTAINING SOLIDS: RENEWABLE PRODUCTION OF BIO-PLASTICS

The present disclosure is related to silica-based Lewis acid catalysts, being essentially devoid of strong Brønsted acid character, and their ability to effect the [4+2] cycloaddition and dehydrative aromatization of dienes and dienophiles containing oxygenated substituents to form substituted benzene products. In some embodiments, the processes comprise contacting biomass-derived substrates with ethylene to form terephthalic acid and its derivatives. 2. The method of claim 1 , wherein the at least one of R claim 1 , R′ claim 1 , R claim 1 , R′ claim 1 , R claim 1 , R′ R claim 1 , R′ claim 1 , R claim 1 , and Ris an oxygenated functional group3. The method of claim 2 , wherein the oxygenated functional group is an acetal claim 2 , aldehyde [—C(O)H] claim 2 , protected aldehyde claim 2 , acyl [—C(O)-(alkyl)] claim 2 , protected acyl claim 2 , hydroxycarbonyl [—C(O)OH] claim 2 , alkoxycarbonyl [—C(O)O-(alkyl)] claim 2 , hydroxymethyl [—CHOH] or alkoxymethyl [—CHO(alkyl)].4. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst comprises a microporous material.5. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst comprises a mesoporous material6. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst comprises amorphous silica.7. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst comprises mesoporous silica.8. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst is a molecular sieve.9. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst is a silica-based molecular sieve having a 10-membered ring topology10. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst is a silica-based molecular sieve having a *BEA topology.11. The process of claim 1 , wherein the solid silica-based Lewis-acid catalyst comprises Ge claim 1 , Hf claim 1 , Nb claim 1 , Sn claim 1 , Ta claim 1 , Ti claim 1 , Zr claim 1 , or a combination ...

COMPOUND HAVING PERFLUOROALKYL TERMINAL GROUP AND CF2O BONDING GROUP, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE

Subject 2. The compound according to , wherein in formula (1a) according to , ring Ais 1 ,4-phenylene , 1 ,4-phenylene in which at least one hydrogen has been replaced by fluorine or chlorine , naphthalene-2 ,6-diyl or naphthalene-2 ,6-diyl in which at least one hydrogen has been replaced by fluorine or chlorine.4. The compound according to , wherein in formula (1b) according to , Ris alkyl having 1 to 15 carbons , alkoxy having 1 to 14 carbons , alkenyl having 2 to 15 carbons or alkenyloxy having 2 to 14 carbons; and Zand Zare independently a single bond , —CHCH— , —CH═CH— , —CFO— or —COO—.6. The compound according to , wherein in formulas (1-1) to (1-4) according to , Ris alkyl having 1 to 15 carbons or alkenyl having 2 to 15 carbons.9. The compound according to , wherein in formulas (1-38) to (1-45) according to , Ris alkyl having 1 to 10 carbons; Land Lare fluorine; and Y , Y , Y , Y , Yand Yare independently hydrogen or fluorine.10. A liquid crystal composition including at least one of compounds according to .15. The liquid crystal composition according to claim 10 , further including at least one additive selected from the group of a polymerizable compound claim 10 , a polymerization initiator claim 10 , a polymerization inhibitor claim 10 , an optically active compound claim 10 , an antioxidant claim 10 , an ultraviolet light absorber claim 10 , a light stabilizer claim 10 , a thermal stabilizer claim 10 , a coloring matter and an antifoaming agent.16. A liquid crystal display device including the liquid crystal composition according to . The invention relates to a liquid crystal compound, a liquid crystal composition and a liquid crystal display device. It relates especially to a liquid crystal compound having a perfluoroalkyl terminal group and a CFO bonding group, a liquid crystal composition including this compound and having a nematic phase, and a liquid crystal display device including this composition.A liquid crystal display device has been widely ...

Method for Separating Optically Active Hydroxy Cineole Derivatives

The present invention relates to a method for separating an optically active hydroxy cineole derivatives by lixiviation and crystallization and enantiomerically pure optically active hydroxy cineole derivatives of purity greater than 99.5% that have been prepared by this process. The present invention further relates to use of the desired enantiomer having enantiomeric excess of at least 99.5% ee as prepared according to the present invention, for the synthesis of enantiomerically pure 7-oxabicyclo[2.2.1]heptane derivatives. 113-. (canceled)15. The method of claim 14 , further comprising adding seed crystals of the desired enantiomer in step (ii).16. The method of claim 14 , wherein{'sup': '1', 'sub': 1', '6', '2, 'Ris selected from the group consisting of hydrogen and C-C-alkyl; wherein alkyl is straight-chain or branched, unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, CN, NO, methyl, phenyl and benzyl; and'}{'sup': '2', 'sub': 1', '6', '2, 'Ris selected from the group consisting of hydrogen and C-C-alkyl; wherein alkyl is straight-chain or branched, unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, CN, NO, methyl, phenyl and benzyl.'}17. The method of claim 16 , wherein Ris methyl and Ris isopropyl.18. The method of claim 14 , wherein the desired enantiomer is either the optically active hydroxy cineole derivative of formula (I-R) or the optically active hydroxy cineole derivative of formula (I-S).19. The method of claim 14 , wherein in step (ii) the suspension is stirred at temperature in the range of ≥10 to ≤120° C.20. The method of claim 14 , wherein in step (iii) the isolation of the crystals of the desired enantiomer is carried out at temperature in the range of ≥−10 to ≤30° C.21. The method of claim 14 , wherein in step (iii) the desired enantiomer is isolated by a method selected from the group consisting of filtration or ...

METHOD FOR SELECTIVELY PREPARING EVOGLUCOSENONE (LGO) AND OTHER ANHYDROSUGARS FROM BIOMASS IN POLAR APROTIC SOLVENTS

A method to produce 5-hydroxymethylfurfural (HMF) is described in which a reactant including cellulose, lignocellulose, or a combination thereof, in a reaction mixture of a polar, aprotic solvent and an acid is reacted for a time, at a temperature, and at a hydrogen ion concentration wherein at least a portion of the cellulose or lignocellulose present in the reactant is converted to HMF. The reaction mixture is initially substantially devoid of water. As the reaction proceeds, dehydration of intermediates causes the water concentration in the reaction mixture to rise to no more than about 2.0 wt % water. 1. A method to produce levoglucosenone (LGO) , the method comprising:reacting a reactant comprising cellulose, lignocellulose, cellobiose, glucose, or a combination thereof, in a reaction mixture comprising a polar, aprotic solvent and an acid, for a time, at a temperature, and at a hydrogen ion concentration wherein at least a portion of the cellulose, lignocellulose, cellobiose, or glucose present in the reactant is converted to LGO.2. The method of claim 1 , wherein the acid is present in an amount to yield a hydrogen ion concentration in the reaction mixture of from about 5 mM to about 500 mM.3. The method of claim 1 , wherein the acid is present in an amount to yield a hydrogen ion concentration in the reaction mixture of from about 5 mM to about 100 mM.4. The method of claim 1 , wherein the acid is present in an amount to yield a hydrogen ion concentration in the reaction mixture of from about 5 mM to about 50 mM.5. The method of claim 1 , wherein the acid is a Brønsted-Lowry Acid.6. The method of claim 1 , wherein the acid is a mineral acid.7. The method of claim 1 , wherein the temperature is from about 80° C. to about 500° C.8. The method of claim 1 , wherein the temperature is from about 80° C. to about 400° C.9. The method of claim 1 , wherein the temperature is from about 80° C. to about 300° C.10. The method of claim 1 , wherein the temperature is from ...

Sugar Derivatives Comprising Sulfur-Containing Moieties And Methods Of Making Same And Methods Of Using The Same For The Treatment Of MPS IIIC

Described herein are modified sugar, iminosugar and azasugar compounds and methods of making same. One or more of these modified compounds contain sulfates, sulfites, sulfamates and/or sulfonamides. Also described are pharmaceutical compositions/formulations comprising these compounds, as well as methods using these modified sugar compounds for the treatment of MPS IIIC (also known as Sanfilippo Type C). 7. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. the compound of ; and'}b. at least one pharmaceutically acceptable carrier.8. A method of making a pharmaceutical composition according to , the method comprising , adding to at least one pharmaceutically acceptable carrier to the compound of .9. A method of making the compound according to claim 4 , the method comprising reacting N-benzyl(N-acetyl 1 claim 4 ,2 deoxynojiimycin) with SOCland pyridine.10. A method of making the compound having a structure represented by formula (V) according to claim 6 , the method comprisinga. reacting 1-deoxygalactonojirimycin with EtOCOCl to produce an intermediate; and{'sub': '2', 'b. reacting the intermediate with SOCl and pyridine.'}11. A method of making the compound having a structure represented by formula (VI) according to claim 6 , the method comprisinga. reacting 1-deoxygalactonojirimycin with EtOCOCl to produce an intermediate; and{'sub': 2', '2, 'b. reacting the intermediate with SOCland pyridine.'}12. A method of making the compound having a structure represented by formula (VII) according to claim 6 , the method comprisinga. reacting 1-deoxynojirimycin with EtOCOCl to produce an intermediate; and{'sub': 2', '2, 'b. reacting the intermediate with SOCland pyridine.'}17. A method of preventing and/or treating MPS IIIC claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of the compound of .18. The method of claim 17 , further comprising administering an effective amount ...

Herbicidally active (alkynyl-phenyl)-substituted cyclic dione compounds and derivatives thereof

The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; Ris fluorine or bromine; Ris ethynyl, C-Calkoxy, C-Chaloalkoxy, or C-Calkoxy-C-Calkoxy-; and Q is a pyran-3,5-dione-4-yl, a thiopyran-3,5-dione-4-yl, a piperidine-3,5-dione-4-yl, a cyclopentane-1,3-dione-2-yl, a cyclohexane-1,3, 5-trione-2-yl, a cyclohexane-1,3-dione-2-yl, or a cycloheptane-1,3-dione-2-yl, or a derivative thereof (e.g. a fused such as fused bicyclic derivative, and/or a spirocyclic derivative), or an enol ketone tautomer derivative thereof, wherein Q is further defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. Preferably, X is methyl; and/or Ris fluorine; and/or Ris —O—R, wherein Ris methyl, ethyl, trifluoromethyl, difluoromethyl, trifluoroethyl, or —CHCHOCH. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the weeds and/or to the plants and/or to the locus thereof. 2. A compound according to wherein X is methyl.3. A compound according to wherein Ris fluorine.4. A compound according to claim 1 , wherein Ris —O—R claim 1 , and wherein Ris methyl claim 1 , ethyl claim 1 , trifluoromethyl or difluoromethyl.5. A compound according to claim 1 , wherein Ris —O—R claim 1 , and wherein Ris methyl.6. A compound according to claim 1 , wherein G is hydrogen; an agriculturally acceptable metal claim 1 , or an agriculturally acceptable sulfonium or ammonium group; or G is —C(X)—Ror —C(X)—X—R.7. A compound according to claim 1 , wherein R claim 1 , Rand Rare hydrogen; or claim 1 ,{'sup': 3', '5', '4', '6', '11', '12', '13', '14', '15', '16', '17', '18', '11', '12', '13', '15', '17', '18, 'Rand Rare hydrogen, and Rand Rtaken together are —C(R)(R)—C(R)(R)— ...

NEW CYCLOADDUCT PRECURSORS OF DIHALODIPHENYLSULFONES AND PREPARATIONS THEREOF

The invention relates to new compounds of formula (I) wherein X represents a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine, which are useful for the preparation of 4,4′dihalodiphenylsulfones of formula (III) wherein X is as defined above. 2. The compound according to claim 1 , wherein the halogen atom is chlorine or bromine claim 1 , preferably chlorine.4. The process according to claim 3 , wherein the halofuran is 3-chlorofuran or 3-bromofuran.5. The process according to claim 3 , wherein the molar ratio of the halofuran of formula (II) to divinylsulfone is of at least 2/1.6. (canceled)8. The process according to claim 7 , wherein the dehydration/aromatization is carried out in the presence of an alkali hydroxide.9. The process according to claim 7 , wherein the dehydration/aromatization is carried out in the presence of DMSO.12. (canceled)15. The process according to claim 13 , wherein the process comprises the step ii) of isolating the 4 claim 13 ,4′-dihalodiphenylsulfone.16. The compound according to claim 2 , wherein the halogen atom is chlorine.17. The process according to claim 8 , wherein the alkali hydroxide is sodium hydroxide or potassium hydroxide.18. The process according to claim 14 , wherein the aminating agent is ammonia.19. A process for forming a shaped article claim 13 , the process comprising solution processing or melt processing the polyarylethersulfone manufactured by the process according to .20. A shaped article formed by the process according to . This application claims priority to European application No. 17306053.4 filed on Aug. 7, 2017, the whole content of this application being incorporated herein by reference for all purposes.The present invention pertains, as new and useful chemical compounds, to specific di-(halo-oxanorbomene)sulfones, obtainable by cycloaddition between a divinylsulfone and a halofuran (Diels-Alder reaction) and to their use as precursors for the preparation of ...

ORTHOESTER COMPOUND

A compound is provided that is useful for, among other things, preparing water-soluble polymer derivatives bearing a terminal N-succinimidyl ester. 1. A compound having the following structure: This application is a continuation of U.S. patent application Ser. No. 13/856,704, filed Apr. 4, 2013, which is a continuation of U.S. patent application Ser. No. 13/453,769, filed Apr. 23, 2012, now U.S. Pat. No. 8,435,504, which is a continuation of U.S. patent application Ser. No. 12/496,294, filed Jul. 1, 2009, now U.S. Pat. No. 8,182,801, which is a continuation of U.S. patent application Ser. No. 10/659,735, filed Sep. 9, 2003, now U.S. Pat. No. 7,569,214, which application claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 60/409,348, filed Sep. 9, 2002, the disclosures of which are incorporated herein by reference.The present invention relates generally to novel methods for preparing polymer derivatives that comprise a terminal carboxylic acid or ester thereof. In addition, the invention relates to polymers, conjugates of the polymers, conjugation methods, and intermediates as well as methods for preparing the intermediates. Furthermore, the invention relates to pharmaceutical preparations, synthetic methods, and the like.Conjugating a water-soluble polymer such as poly(ethylene glycol) (or “PEG”) to a biologically active agent results in a polymer-active agent conjugate that often has advantageous properties over the corresponding “unconjugated” version of the active agent. Among other advantages, conjugated forms of active agents have increased half-lives and are less immunogenic. When PEG is used to form a polymer-active agent conjugate, the conjugated active agent is conventionally referred to as “PEGylated.” Commercially available PEGylated preparations include PEGASYS® PEGylated interferon alpha-2a (Hoffmann-La Roche, Nutley, N.J.), PEG-INTRON® PEGylated interferon alpha-2b (Schering Corp., Kennilworth, N.J.), NEULASTA™ PEG-filgrastim ...

Compound and Preparation Method Thereof

Disclosed is a compound, prepared by extracting and separating from Limax. Also disclosed is a method for extracting and separating the compound, which is simple and easy to operate. The compound has sedative and hypnotic effects, and has significant effects on physiological or psychological dependent detoxification or detoxication. It has potential application value for preparing detoxification or detoxication drugs, and provides new ideas for the further development of detoxification drugs. 2. The compound according to claim 1 , wherein the compound has a molecular formula: CHO; molecular weight: 524; melting point: 248-249° C.; solubility: white needle-like or columnar crystal claim 1 , insoluble in water claim 1 , insoluble in acid and alkali claim 1 , easily soluble in methanol claim 1 , acetone claim 1 , soluble in ethanol claim 1 , ethyl acetate claim 1 , hot trichloromethane claim 1 , and slightly soluble in cold trichloromethane.3. The compound according to claim 1 , wherein the chiral C configurations of the compound comprises: C3 claim 1 , R; C6 claim 1 , S; C7 claim 1 , S; C10 claim 1 , S; C11 claim 1 , R; C12 claim 1 , R; C13 claim 1 , R; C14 claim 1 , R; C15 claim 1 , S; C18 claim 1 , S; C19 claim 1 , S; and C22 claim 1 , R.4. The compound according to claim 1 , wherein the compound is prepared by extracting and separating from Limax.5. The compound according to claim 4 , wherein the Limax comprise one or more of Vaginulus alte (Ferussac) claim 4 , Limax maximus L. claim 4 , L. flavus L. claim 4 , Agriolimax agrestis L. claim 4 , and Phiolomycus bilineatus.6. A method for preparing the compound according to claim 1 , comprising the following steps:S1. pulverizing Limax to obtain Limax powder;{'sub': '2', 'S2. putting the Limax powder into a supercritical COextractor for extraction to obtain an extract;'}S3. adding the extract, potassium hydroxide, and water to a reactor in a weight ratio of “extract:potassium hydroxide:water=1:1:1.5”, mixing evenly, ...

ORIDONIN FUNCTIONALIZED SELENIUM NANOPARTICLES AND METHOD OF PREPARATION THEREOF

The present invention relates to an oridonin functionalized selenium nanoparticle, method of preparing and use thereof for anti-cancer and anti-inflammatory treatments. The present invention provides oridonin functionalized selenium nanoparticle that is stable, water soluble and storable. 1. A method of preparing oridonin functionalized selenium nanoparticle comprises:a) Providing a solution of selenium-containing compound, a solution of oridonin, a solution of reducing agent and a solution of stabilizer;b) Mixing the solutions of selenium-containing compound, oridonin, and stabilizer to form a first mixture;c) Adding the solution of reducing agent to the first mixture to form the nanoparticle,wherein the oridonin functionalized selenium nanoparticle comprises 0.01-10 mM selenium, 0.01-10 mM oridonin, 0.001%-10% stabilizer and 0.1-100 mM reducing agent.2. The method of claim 1 , wherein the selenium-containing compound comprises selenite claim 1 , salt of selenite claim 1 , selenite acid claim 1 , selenium thiosulfate claim 1 , selenium dioxide or a combination thereof.3. The method of claim 1 , wherein the reducing agent comprises ascorbic acid claim 1 , gallic acid claim 1 , asparagine claim 1 , sodium sulphite or a combination thereof.4. The method of claim 1 , wherein the stabilizer comprises chitosan claim 1 , hyaluronic acid claim 1 , sodium hyaluronate claim 1 , or a cellulose derivative or a combination thereof.5. The method of further comprises allowing the solutions of selenium-containing compound claim 1 , oridonin claim 1 , stabilizer and reducing agent to mix until color intensity in the solution mixture stops increasing claim 1 , wherein the stopping of the increase in color intensity indicates completion of formation of nanoparticle.6. An optimization oridonin functionalized selenium nanoparticle prepared by the method of .7. The oridonin functionalized selenium nanoparticle of claim 6 , wherein the nanoparticle has an average particle size of 35-160 ...

PYRANOCHROMENYL PHENOL DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR TREATING METABOLIC SYNDROME OR INFLAMMATORY DISEASE

Provided are a pyranochromenyl phenol derivative, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also provided is a pharmaceutical composition for preventing or treating metabolic syndrome or inflammatory disease comprising same. 2. The compound of Formula (1) claim 1 , the pharmaceutically acceptable salt thereof claim 1 , or the solvate thereof of claim 1 , wherein Ris a hydrogen atom claim 1 , and Ris a hydrogen atom; a straight or branched C-Calkyl group; a straight or branched C-Calkoxy group; or a straight or branched C-Cthioalkyl group.3. The compound of Formula (1) claim 2 , the pharmaceutically acceptable salt thereof claim 2 , or the solvate thereof of claim 2 , wherein Ris a hydrogen atom claim 2 , and Ris methyl claim 2 , ethyl claim 2 , n-propyl claim 2 , n-butyl claim 2 , ethoxy claim 2 , n-propoxy claim 2 , n-butoxy or methoxymethoxy.6. The pharmaceutical composition of claim 5 , wherein in Formula (I′) claim 5 , Ris a hydrogen atom claim 5 , and Ris a hydrogen atom; a hydroxy group; a straight or branched C-Calkyl group; a straight or branched C-Calkoxy group; or a straight or branched C-Cthioalkyl group.7. The pharmaceutical composition of claim 6 , wherein in Formula (I′) claim 6 , R1 is a hydrogen atom claim 6 , and Ris methyl claim 6 , ethyl claim 6 , n-propyl claim 6 , n-butyl claim 6 , ethoxy claim 6 , n-propoxy claim 6 , n-butoxy or methoxymethoxy.9. The pharmaceutical composition of claim 5 , wherein the metabolic syndrome is one or more of obesity claim 5 , diabetes claim 5 , hyperlipidemia claim 5 , and fatty liver.10. The pharmaceutical composition of claim 9 , wherein the diabetes is type 2 diabetes mellitus.11. The pharmaceutical composition of claim 5 , wherein the metabolic syndrome is a complex disease of type 2 diabetes mellitus and obesity.13. The pharmaceutical composition of claim 12 , wherein in Formula (I′) claim 12 , Ris a hydrogen atom claim 12 , and Ris a hydrogen atom; a hydroxy group; a straight or ...

ANTIVIRAL COMPOSITION AND METHOD FOR CONTROLLING PLANT VIRUSES USING THE SAME

Disclosed are an antiviral composition, a composition for controlling plant viruses, and a method for controlling plant viruses using the composition. Trichodermin or Trichoderminol which is a tricothecene-based compound and is isolated from strain has antiviral activities against various plant viruses and is thus suitable for controlling plant viruses. This description can facilitate mass production of an active component derived from natural products, provide environment-friendly antifungal agents, which do not harm plants, using safe materials, and be variously utilized in agricultural fields, for example, such as production of high-value crops.

PROCESS FOR PREPARING BICYCLIC ENOLETHER

Described herein is a process for preparing a compound of formula (I) starting from a compound of formula (II), where the process is catalyzed by a Ruthenium complex. 2. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.3. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.4. The process according to according to claim 1 , characterized in that Rrepresents a 1 claim 1 ,2-propanediyl group or 1 claim 1 ,2-ethanediyl group.5. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.6. The process according to claim 1 , characterized in that Rrepresents a linear or branched Calkanediyl group.7. The process according to claim 1 , characterized in that Rrepresents a 1 claim 1 ,8-octanediyl group.8. The process according to claim 1 , characterized in that compound of formula (I) is selected from the group consisting of 12-oxabicyclo[6.3.1]dodec-8-ene claim 1 , 10-methyl-12-oxabicyclo[6.3.1]dodec-8-ene claim 1 , 13-oxabicyclo[7.3.1]tridec-9-ene claim 1 , 11-methyl-13-oxabicyclo[7.3.1]tridec-9-ene claim 1 , 14-oxabicyclo[8.3.1]tetradec-10-ene claim 1 , 12-methyl-14-oxabicyclo[8.3.1]tetradec-10-ene claim 1 , 15-oxabicyclo[9.3.1]pentadec-11-ene claim 1 , 13-methyl-15-oxabicyclo[9.3.1]pentadec-11-ene claim 1 , 16-oxabicyclo[10.3.1]hexadec-12-ene claim 1 , 14-methyl-16-oxabicyclo[10.3.1]hexadec-12-ene claim 1 , 17-oxabicyclo[11.3.1]heptadec-13-ene claim 1 , and 15-methyl-17-oxabicyclo[11.3.1]heptadec-13-ene.9. The process according to claim 1 , characterized in that compound of formula (II) is selected from the group consisting of cycloundecane-1 claim 1 ,5-dione claim 1 , 3-methylcycloundecane-1 claim 1 ,5-dione claim 1 , cyclododecane-1 claim 1 ,5-dione claim 1 , 3-methycyclododecane-1 claim 1 ,5-dione claim 1 , cyclotridecane-1 claim 1 ,5-dione claim 1 , 3-methycyclotridecane-1 claim 1 ,5-dione claim 1 , ...

1-OXO/ACYLATION-14-ACYLATED ORIDONIN DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylated-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs. 2. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein W is oxo or formyloxy.3. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the aryl is phenyl.4. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the heteroaryl is a five-membered or six-membered aromatic ring group containing oxygen claim 1 , nitrogen claim 1 , or sulfur heteroatom.5. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 4 , wherein the heteroaryl is furyl claim 4 , thienyl claim 4 , pyrrolyl claim 4 , or pyridyl.6. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the aryl claim 1 , heteroaryl claim 1 , C-Ccycloalkyl claim 1 , C-Ccycloalkenyl and heterocyclyl are respectively optionally substituted with a substituent selected from the group consisting of halogen claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Calkylthio claim 1 , and C-Calkyl.7. The 1-oxo/acylated-14-acylated oridonin derivative or a pharmaceutically acceptable salt thereof according to claim 6 , wherein the substituent is fluoro claim 6 , chloro claim 6 , bromo claim 6 , nitro claim 6 , cyano claim 6 , methoxy claim 6 , ethoxy claim 6 , propoxy claim 6 , methyl claim 6 , ethyl claim 6 , propyl claim 6 , isopropyl claim 6 , ...

INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS

The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections. 2. The compound of wherein the compound is selected from the group consisting of claim 1 , VT-03-00014: 4-(2-(3-([1 claim 1 ,3]oxathiolo[5 claim 1 ,4-c]pyridin-6-ylmethylamino)-8 azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00017: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methylbenzenesulfonamide; VT-03-00021: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxine-6-sulfonamide; VT-03-00021a: 4-(2-(3-((2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxin-6-yl)methylamino)-8azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00022: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)naphthalene-2-sulfonamide; VT-03-00024: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxine-6-carboxamide; VT-03-00026: 6-methoxy-4-(2-(3-((3-oxo-3 claim 1 ,4-dihydro-2H-benzo[b][1 claim 1 ,4]thiazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)quinoline-3-carbonitrile; VT-03-00026a: 4-(2-(3-((3 claim 1 ,4-dihydro-2H-benzo[b][1 claim 1 ,4]thiazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00027: 4-(2-(3-((2 claim 1 ,3-dihydro-[1 claim 1 ,4]dioxino[2 claim 1 ,3-c]pyridin-7-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00028: 4-(2-((1R claim 1 ,4R)-5-((2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxin-6-ylamino)methyl)-2 claim 1 ,5-diazabicyclo[2.2.1]heptan-2-yl)ethyl)-6-methoxyquinoline-3-carbonitrile;VT-03-00030: 6-methoxy-4-(2-(3-((3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)quinoline-3-carbonitrile; VT-03-00031: 4-(2 ...

CHIRAL AUXILIARIES AND USES THEREOF

The present invention relates to chiral auxiliaries and the syntheses thereof and uses thereof. 6. An enantiomerically enriched compound according to claim 1 , wherein one of Rand Ris optionally substituted aryl or optionally substituted arylalkyl.7. An enantiomerically enriched compound according to claim 1 , wherein one of Rand Ris optionally substituted benzyl.8. An enantiomerically enriched compound of claim 7 , wherein one of Rand Ris optionally substituted benzyl and is in a syn-relationship with respect to X.9. An enantiomerically enriched compound according to claim 1 , wherein Rand Rare each independently substituted with one or more alkyl groups.10. An enantiomerically enriched compound according to claim 1 , wherein Rand Rare each independently substituted with one or more halogen groups.11. An enantiomerically enriched compound according to claim 1 , wherein Rand Rtaken together form a spirocyclic compound.12. An enantiomerically enriched compound according to claim 1 , wherein X is OH.15. A process according to claim 14 , wherein the process further comprises the step of epimerising the compound of formula (IIIb).16. An enantiomerically enriched compound prepared according to the process of .17. A method of using the enantiomerically enriched compound according to as a chiral auxiliary to control the stereochemical outcome of a cycloaddition or a conjugate addition reaction.18. The method according to claim 17 , wherein the reaction is a cycloaddition reaction claim 17 , which is a Diels-Alder reaction.19. The method according to claim 18 , wherein a suitable Lewis acid catalyst is used.20. The method according to claim 19 , wherein the Lewis acid catalyst is selected from the group consisting of SnCl claim 19 , AlCl claim 19 , TiCl claim 19 , BF claim 19 , EtAlCl and EtAlCl.21. A method of using the enantiomerically enriched compound according to as a resolving agent to separate an enantiomer of a compound from a mixture of its enantiomers.22. A method ...

Method for Preparing Curable Bicyclic Compound Derived from Biomass

The present invention relates to a curable bicyclic compound derived from biomass, solvent-free curable composition and a method for preparing thereof. The curable compound derived from biomass according to the invention comprises a bicycle structure, to which one of two epoxide functional groups are bonded. 110-. (canceled)11. A method for preparing a curable bicyclic compound derived from biomass , the method comprising:a step of preparing starting materials by preparing furan from hemicellulose extracted from biomass, and methyl acrylate from glycerol generated from biomass;a step of preparing an intermediate compound comprising bicycle and an alcohol functional group by reacting the starting materials; anda step of preparing a curable bicyclic compound comprising bicycle and an epoxide functional group by reacting the Intermediate compound and epichlorohydrin.12. The method according to claim 11 , wherein the step of preparing an intermediate compound involves reducing the intermediate compound by hydrogenation.13. The method according to claim 11 ,wherein the step of preparing a curable bicyclic compound involves reacting a mixture comprising the intermediate compound and the epichlorohydrin using PTC (Phase Transfer Catalyst) as a catalyst in a bi-phasic solvent system where a sodium hydroxide aqueous solution is added.14. The method according to claim 11 , wherein the step of preparing an intermediate compound prepares an intermediate compound comprising bicycle and one alcohol functional group by reacting the furan and the methyl acrylate through Diels-Alder reaction and consecutive reduction claim 11 , and the step of preparing the curable bicyclic compound prepares the curable bicyclic compound comprising bicycle and one epoxide functional group by reacting the intermediate compound and epichlorohydrin.15. The method according to claim 14 , wherein the step of preparing an intermediate compound involves separating the compound formed after the Diels-Alder ...

TAXANE COMPOUND, AND PREPARATION METHOD AND USE THEREOF

Provided are taxanes compounds having the structure of formula I, preparation method thereof, and uses of compositions having the compound, pharmaceutical salts and solvates thereof as active ingredients in the preparation of oral antitumor drugs. In the formula, Ris —COR, —COOR, and —CONRR; Ris C1-C6 alkyl, C1-C6 alkenyl group, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; Ris —OR, —OCOOR, —OCOSR, and —OCONRR; Ris —OR, —OCOOR, —OCOSR, —OCONRR, H, and OH; Ris C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl group, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; and Rand Rare respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. 4. The taxanes compounds according to claim 1 , wherein said taxanes compounds further include all isomers of these compounds and mixtures of the isomers.5. The taxanes compounds according to claim 1 , wherein said taxanes compounds are formed into pharmaceutically acceptable non-toxic salts.6. The taxanes compounds according to claim 1 , wherein said taxanes compounds exist in a form of solvates.7. An antitumor pharmaceutical composition claim 1 , wherein the composition contains the taxanes compounds with formula I according to claim 1 , pharmaceutically acceptable salts or solvates thereof as active ingredients.8. The composition according to claim 7 , wherein the pharmaceutical composition contains the taxanes compounds with formula I claim 7 , pharmaceutically acceptable salts or solvates thereof in a weight ratio of 0.01% to 99.99% with the balance of pharmaceutically acceptable carriers.9. Use of the taxanes compounds according to claim 1 , pharmaceutically acceptable salts claim 1 , solvates thereof in manufacturing oral antitumor medicaments.10. A preparation method of the taxanes compounds according to claim 1 , characterized in that claim 1 , the method comprises the following steps:Step 1 synthesis of ...

SANDWICH ASSAY DESIGN FOR SMALL MOLECULES

Methods are disclosed of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2,000. The method comprises preparing a first antibody that binds to the small molecule, and preparing a second antibody that binds to the small molecule at a portion of the small molecule other than a portion to which the first antibody binds. The second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule. The antibodies may be employed in sandwich assays for the small molecule. 1. A method of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2 ,000 , the method comprising:(a) preparing a first antibody that binds to the small molecule, and(b) preparing a second antibody that binds to the small molecule in a portion of the small molecule other than a portion to which the first antibody binds, wherein the second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule.2. The method according to wherein the first antibody is prepared from an immunogen that comprises a portion of the small molecule other than the predetermined portion.3. The method according to wherein the predetermined portion of the small molecule is obtained by modification of the small molecule to alter a spatial conformation of the small molecule.4. The method according to wherein the predetermined portion of the small molecule is a compound that consists essentially of the predetermined portion.5. The method according to wherein the small molecule is a macrolide.6. The method according to wherein the small molecule is an immunosuppressant drug.7. The method according to wherein one or both of the first antibody and the second antibody are monoclonal antibodies.8. A method of determining a presence and/or amount of a small molecule having a molecular weight of about 500 to about 2 claim 1 ,000 in a sample ...

CORTISTATIN ANALOGUES AND SYNTHESES THEREOF

The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: 2. The compound of claim 1 ,wherein:each of the dashed lines independently represents the presence or absence of a bond;n is 2;m is 1;{'sub': '1', 'Ris unsubstituted heteroaryl;'}{'sub': 2', '1', '6, 'Ris C-Caliphatic;'}{'sub': '3', 'Ris hydrogen; and'}{'sub': '4', 'each occurrence of Ris independently selected from the group consisting of halogen; cyclic or acyclic, unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, unsubstituted, branched or unbranched heteroaliphatic; unsubstituted, branched or unbranched acyl;'}{'sub': D', 'D', '2', 'D', 'D', 'D', '2', 'D', '2', '3', 'D', 'D', '2', 'D', 'A', 'D', '2', 'D', 'D', 'D', '2', 'D', 'D', 'D', '3', 'A', 'D, 'unsubstituted aryl; unsubstituted heteroaryl; —OR; —C(═O)R; —COR; —CN; —SCN; —SR; —SOR; —SOR; —NO; —N; ═O; ═N(R); ═S; —N(R); —NHC(═O)R; —NRC(═O)N(R); —OC(═O)OR; —OC(═O)R; —OC(═O)N(R); —NRC(═O)OR; and —C(R); wherein each occurrence of Rand Ris independently selected from the group consisting of hydrogen; a protecting group attached to a nitrogen, oxygen or sulfur atom; aliphatic; heteroaliphatic; acyl; aryl; heteroaryl; alkoxy; aryloxy; alkylthio; arylthio; amino; alkylamino; dialkylamino; heteroaryloxy; and heteroarylthio.'}3. The compound of claim 2 , wherein each occurrence of Ris independently selected from the group consisting of halogen; cyclic or acyclic claim 2 , unsubstituted claim 2 , branched or unbranched aliphatic; cyclic or acyclic claim 2 , unsubstituted claim 2 , branched or unbranched heteroaliphatic; unsubstituted claim 2 , branched or unbranched acyl; unsubstituted aryl; unsubstituted heteroaryl; —OR; —C(═O)R; —COR; —CN; —SCN; —SR; —SOR; —SOR; —NO; —N; ═O; ═N(R); ═S; —N(R); —NHC(═O)R; —NRC(═O)N(R); —OC(═O)OR; —OC(═O)R; —OC(═O)N(R); —NRC(═O)OR; and —C(R); wherein each occurrence of Rand Ris independently selected from the group consisting of hydrogen; aliphatic; heteroaliphatic; acyl; ...

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials. 4: The compound according to claim 1 , wherein G3 is N claim 1 , CH or C(CH).5: The compound according to claim 1 , wherein Ris hydrogen atom claim 1 , halogen atom claim 1 , cyano claim 1 , (C)alkyl or NR′R″ claim 1 , wherein R′ and R″ are hydrogen atom or (C)alkyl.6: The compound according to claim 1 , wherein Ris hydrogen atom claim 1 , F claim 1 , Cl claim 1 , cyano claim 1 , CH claim 1 , NHor N(CH).7: The compound according to claim 1 , wherein said Ris hydrogen atom claim 1 , fluorine atom claim 1 , chloride atom claim 1 , OH claim 1 , (C)alkyl-OH claim 1 , —COOR′ or —CON(R′)(R″) claim 1 , wherein R′ and R″ claim 1 , identical or different each other claim 1 , are hydrogen atom or (C)alkyl.8: The compound according to claim 1 , wherein said Ris hydrogen atom claim 1 , halogen atom claim 1 , cyano claim 1 , (C)alkyl claim 1 , (C)alkoxy claim 1 , or NR′R″ claim 1 , wherein R′ and R″ claim 1 , identical or different each other claim 1 , are hydrogen atom or (C)alkyl.9: The compound according to claim 1 , wherein said Y is (C)alkylenyl group claim 1 , —NH—(C)alkylenyl group or (C)cycloalkylenyl group claim 1 , said group being optionally substituted with one hydroxy group or an amino group.10: The compound according to claim 1 , wherein said Pis O claim 1 , S claim 1 , SOor CH.11: The compound according to claim 1 , wherein said Rand Rtogether form a 5- or 6-membered aromatic or aliphatic ring claim 1 , optionally comprising at least one heteroatom selected from N claim 1 , O and S claim 1 , wherein said ring optionally bears an oxo group.12: The compound according to claim 11 , wherein Rand Rtogether form a 6-membered ring selected from benzene or pyridine.13: A pharmaceutical composition claim 1 , comprising at least one compound of formula (I) according to claim 1 , a salt thereof with a pharmaceutically acceptable organic ...

Oxabicycloalkane herbicides

Herbicidal compounds of the general formula wherein X is (-CR 4 R 4 -) m in which m is 0 or 1; Y is (-CR 5 R 6 -) n in which n is 0,1 or 2; Z is (-CR 7 R 7 -) p in which p is 1, 2 or 3; the sum of m + n + p is an integer of from 2 to 5; R, is a hydrogen atom or a C 1-6 alkyl group optionally substituted by up to 3 fluorine, chlorine and/or bromine atoms; R 2 is a hydrogen atom or a C 1-6 straight-chain alkyl group; R 3 is a hydrogen atom; a C 1-10 alkyl group; a cyano group; an alkyl group substituted by one or more halogen atoms or by a hydroxy group, a cyano group, a C 1-6 alkoxy group, an aryloxy group, a C 1-6 alkylsulphonyl group, an arylsulphonyl group, an aralkylsulphonyl group, an azido group, a C 1-6 alkoxycarbonyl group, an aralkoxycarbonyl group, a hydroxycarbonyl group, a phosphoryl group, a phosphoryloxy group, or an amine oxide, carbamoyl or thiocarbamoyl group in which each nitrogen is substituted by hydrogen or by 1 or 2 C 1-4 alkyl groups; a C 2 - 4 alkenyl or alkynyl group; an aryl or aralkyl group, each containing from 6 to 11 carbon atoms including 1 to 4 carbon atoms in the alkyl portion and optionally ring substituted by one or more fluorine, chlorine and/or bromine atoms or by a C 1-2 alkyl or alkoxy group, each optionally substituted by one or more fluorine and/or chlorine atoms; a group -CSNH 2 : a group -CO 2 R 8 or -CON(R 8 ) 2 in which R 8 is a hydrogen atom or a C 1-6 alkyl group; or a C 1-6 acyl group or an oxime or an acetal derivative of said acyl group; each R 4 is independently a hydrogen atom; an alkyl group optionally substituted by up to 3 halogen atoms; a hydroxy group; or a C 1-4 alkoxy group; or one of R 4 and R 1 together form a carbon-carbon bond; R 5 and R 6 each independently is a hydrogen atom or a C 1-2 alkyl group; or when located on a carbon atom adjacent to the ring oxygen atom then R 5 and R 6 together form an alkylene group containing 4 or 5 carbon atoms; each R 7 independently is a hydrogen atom or a C 1-4 alkyl ...

Process for the preparation of oxabicyclo alkane derivatives

An oxabicycloalkane derivs of formula (I), useful as selective herbicides, are prepd. by reacting a substd. oxabicycloalkanol of formula (II) with a compd. of formula WCQ2L. In the formulas, X is (-CR4R4-)m [m=0 or 1!; Y is (-CR5R6-)n [n=0, 1 or 2 ; Z is (-CR7R7)p [p=1,2 or3 ; R1 and R2 are each H or C1-6 alkyl; R3 is H, CN, substd. alkyl or acetal deriv.; R4 is H, C1-6 alkyl, hydroxy or C1-4 alkoxy; R5 and R6 are each H or C1-2 alkyl; R7 is H or C1-4 alkyl; Q is H or F; W is alkenyl, alkynyl, opt. substd. aromatic or heterocyclic gp., cycloalkyl, cyclohexenyl, CN or sec. alkyl.

Method of preparing tetrathiafulvalene precursor

FIELD: chemical industry. SUBSTANCE: tetrathiafulvalene (6) derivatives are used as organic conductors, organic superconductors, organic magnetic or like materials. Claimed method of preparing tetrathiafulvalene of formula I: wherein R 1 and R 2 are alkyl, aralkyl, alkene, alkoryl, hydroxyalkyl, trimethylsilyl and trimethylsilylethoxymethyl and when R 1 and R 2 are bonded to form ring, they are alkylene, dimethylenethio, dimethylenoether. Compound 1 is prepared by single reactor and single stage method without generation of difficultly removable by-products and hence with high yield and high purity for short period of time: one of two rings 1,3,4,6-tetrathiapentene -2,5-dione is selectively detached in alcoholic solution containing alkali metal methoxide in inert atmosphere at 30 C or lower. The resulting 1,3-diol-2-one-4,5-dithiolate dianion is reacted with compound having monovalent or divalent group which corresponds to R 1 and R 2 in formula I. Derivatives of formula (I) are prepared using above-indicated stage for preparing precursor and stage of reaction combination of two precursor molecules to obtain tetrathiafulvalene derivative with high yield and for short period of time. EFFECT: more efficient preparation method. 11 cl, 1 dwg, 8 ex ГооОосстс ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2 122 001‘ 13) Сл С 070 339/06, 495/06 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 93054536/04, 29.09.1993 (30) Приоритет: 30.09.1992 ШР 4-262348 (46) Дата публикации: 20.11.1998 (56) Ссылки: ЕР 0281449, 1988. ЕР 0454814, 1990. 1$ 4691028, 1987. (71) Заявитель: Сумитомо Электрик Индастриз, Лтд. (Р) (72) Изобретатель: Харальд Дитмар Мюллер (4Р), Йосинобу Уэба (.Р) (73) Патентообладатель: Сумитомо Электрик Индастриз, Лтд. (ШР) (54) СПОСОБ ПОЛУЧЕНИЯ ПРЕДШЕСТВЕННИКА ТЕТРАТИАФУЛЬВАЛЕНА И СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНОГО ТЕТРАТИАФУЛЬВАЛЕНА (57) Реферат: Производные тетратиафульвалена (6) могут использоваться как ...

메소 화합물을 촉매 비대칭 탈대칭화시키는 방법

본 발명은 프로키랄(prochiral) 출발 물질, 예를 들어 메소 무수물로부터 키랄 비라세미 생성물, 예를 들어 거울상이성질체 부화된 헤미에스테르를 합성하는 방법에 관한 것이다. 또한, 본 발명은 상기 언급된 방법을 위한 촉매, 및 이러한 촉매를 제조하는 방법에 관한 것이다.

Method of producing derivatives of 2,9-dioxatricyclo (4,3,1,03,7) decanone

Method of obtaining 10b-methyl- or 10a-methyl-2,9-dioxatricyclo (4,3,1,0-3-7) decanes

A process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,03,7] decane derivatives is disclosed, wherein a 10-methylen-3-iodomethyl compound of the formula <IMAGE> is hydrogenated to obtain a mixture of the corresponding epimeric 10 beta - and 10 alpha -methyl-3-iodomethyl compounds, the pure 10 alpha - and 10 beta -methyl epimers are separated and recovered from this mixture and are reacted with a secondary amine. Optionally, the substituent in the 4-position of the resulting 10 alpha - or 10 beta -methyl-3-aminomethyl compounds are further changed.

Heterobicycloalkane derivatives

FIELD: organic chemistry. SUBSTANCE: product: heterobicycloalkanes of the formula (I) сС16$90с ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ “” 2 063 972 ' (51) МПК8 С 07 р 493/08, А 01 М 43/24 13) СЛ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5011568/04, 05.05.1992 (30) Приоритет: 22.07.1987 СВ 8717274 07.10.1987 СВ 8723488 26.04.1988 СВ 8809851-2 (46) Дата публикации: 20.07.1996 (56) Ссылки: 1. ЕР М 152229, кл. С 070 49308, опубл. 1985. 2. ЕР М 211538, кл. С 07О 493/08, опубл. 1987. 3. ЕР М 216624, кл. С 070 493/08, опубл. 1987. 4. ЕР М 216625, кл. С ОГО 49308, опубл. 1987. (62) Первичная заявка, из которой выделена настоящая: 4356326/04 (71) Заявитель: Руссель-Юклаф (ЕК) (72) Изобретатель: Джон Бернард Вестон[СВ], Джон Патрик Ларкин[ГСВ], Ян Гарольд Смит[СВ] (73) Патентообладатель: Руссель-Юклаф (ЕК) (54) ПРОИЗВОДНЫЕ ГЕТЕРОБИЦИКЛОАЛКАНОВ (57) Реферат: Использование: в сельском хозяйстве в качестве пестицидов, особенно против членистоногих вредителей. Сущность: продукт-гетероциклоалканов —Фф-лы | С определенными значениями радикалов. Структура соединения ф-лы | приведена в тексте описания. 5 табл. 2063972 С1 КО сС16$90с ПЧ Го (19) КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ 13) ВИ” 2 063 972 Сл 5 С 070 493/08, А 01 М 43/24 (21), (22) АррИсаНоп: 5011568/04, 05.05.1992 (30) РношуУ: 22.07.1987 СВ 8717274 07.10.1987 СВ 8723488 26.04.1988 СВ 8809851-2 (46) Рае ог рибИсаНоп: 20.07.1996 (62) Еа\ег аррйсаНоп: 4356326/04 (71) АррИсапе: Киззе!'-/иКат (ЕК) (72) пуетог. — Охпоп Вегпага МУезюп[СВ], О7Поп Рак Гагкт[СВ], Чап Саго!’а Эт [СВ] (73) Ргорпеюг: Киззе!-уиКаР (ЕК) (54) НЕТЕКОВСУСЕОАЕКАМЕ ОЕКМАТМЕЗ (57) АБзасЕ: НЕГО: огдапс спетгу. ЗОВЗТАМСЕ: ргодис": пыегосусоа!Капез о! Пе Тогтца (1) 1 м Чейпйе гафса| уашез. Зутпезхея сотроуп@$ \меге изея п адпсииге а$ резисае$, езреса!у, адат${ АЙПгороЯя рез{$. ???ЕРЕЕСТ: ипргоуея теоа ог зупез5. 5 15 2063972 С1 КО сС16$90с ПЧ ГЭ Настоящее изобретение относится и ...

Application of substituted 2,3,5,6-tetraoxabicyclo[2,2,1]heptanes as fungicidal agents and fungicidal composition based thereon

FIELD: chemistry. SUBSTANCE: invention relates to substituted 2,3,5,6-tetraoxabicyclo[2.2.1]heptanes of general formula where R=methyl, ethyl, n-butyl, CH 2 C(O)OEt, n-Br-C 6 H 4 CH 2 , the use of these compounds as fungicidal agents and fungicidal compositions based thereon. The compositions consist of substituted 2,3,5,6-tetraoxabicyclo[2.2.1]heptanes of general formula I at a concentration of 0.1-99% and excipients. EFFECT: creating a new class of effective fungicidal agents and the development of fungicidal compositions that will more effectively combat fungal diseases of crops as compared to a commonly used fungicide such as triadimephon. 2 cl, 1 tbl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 627 309 C1 (51) МПК C07D 493/08 (2006.01) A01N 43/02 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2016143326, 03.11.2016 (24) Дата начала отсчета срока действия патента: 03.11.2016 Дата регистрации: (73) Патентообладатель(и): Терентьев Александр Олегович (RU), Ярёменко Иван Андреевич (RU) Приоритет(ы): (22) Дата подачи заявки: 03.11.2016 (45) Опубликовано: 07.08.2017 Бюл. № 22 C 1 2494102 C1, 27.09.2013. Thomas M. Klapotke et al., "Energetic Organic Peroxides-Synthesis and Characterization of 1,4-Dimethyl-2,3,5,6tetraoxadicyclo [2.2.1]heptanes", Eur.J. Organic Chtmistry, 2015, v. 28, p.6237-6242. US 6127405 A, 03.10.2000. (54) Применение замещенных 2,3,5,6-тетраоксабицикло[2.2.1]гептанов в качестве фунгицидных средств и фунгицидная композиция на их основе (57) Реферат: Изобретение относится к химии органических веществ, что позволит более эффективно бороться пероксидов, а именно к замещенным 2,3,5,6с грибковыми заболеваниями тетраоксабицикло[2.2.1]гептанам общей формулы сельскохозяйственных культур по сравнению с I, где R=метил, этил, н-бутил, CH2C(O)OEt, nтаким широко используемым фунгицидом, как триадимефон. 2 н.п. ф-лы, 1 табл., 6 пр. Вr-С6H4СН2, применению этих соединений в R U качестве ...

Method for preparing deoxyelephantolide or isodeoxyelephantolide

本发明公开了一种制备去氧地胆草内酯或异去氧地胆草内酯的方法。本发明提供的方法采用AB‑8大孔树脂初步富集和HSCCC分离纯化，可以制备得到纯度分别为99.6％、99.5％的去氧地胆草内酯、异去氧地胆草内酯，回收率分别达1.05g去氧地胆草内酯/1kg地胆草药材、2.38g异去氧地胆草内酯/1kg地胆草药材，纯度高且回收率高。

Patent JPS5417759B1

Process for preparing 2,9-dioxatricyclo (4,3,1,33.7) decane derivatives

Title compds. (I; R1 = tertiary amine; R2, R3 = H, hydroxy, acyloxy; R4,R5 = H, methyl; R6,R7 = H, alkoxy or aralkoxy) having soporific, sedative activities, were manufd. Thus, hydrogenation of 3-iodomethyl-4β-acetoxy-8-methoxy-10-methylene-2,9-dioxatricyclo(4,3,1,03.7)decane, gave 3-iodomethyl-4-acetoxy-8-methoxy-10β-methyl-2,9-dioxatricyclo(4,3,1,03.7)decane which was reacted with piperidine to give 3-piperidinomethyl-4β-hydroxy-8-methoxy-10β-methyl-2,9-dioxatricyclo-(4,3,1,03.7)decane, which was mixed with L(+)-trataric acid to give 3-piperidinomethyl-4β-hydroxy-8-methoxy-10β-methyl-2,9-dioxatricyclo(4,3,1,03.7)decane hydrogen tartarate.

Method for simultaneously preparing elephantopin and allopatricolone

本发明公开了一种同时制备地胆草内酯、异地胆草内酯的方法。本发明提供的方法利用大孔树脂柱层析和高速逆流色谱可以从地胆草中同时制备得到地胆草内酯、异地胆草内酯，纯度分别为98.9％、99.4％。

Polycyclic compounds and organic electroluminescence device employing the same

Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.

Polycyclic compounds and organic electroluminescence device employing the same

Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.

Polycyclic compound and organic electroluminescent device using the same

중심 벤젠환에 2개의 벤젠환이 축합환을 형성하도록 결합되고, 더욱이 그 말단에 다른 축합환이 결합된 구조를 갖는 화합물의 다환계 화합물, 및, 음극과 양극사이에, 발광층을 포함하는 1층 이상의 유기 박막층을 갖고, 상기 유기 박막층의 적어도 1층이, 본 발명의 다환계 화합물을 함유하는 유기 전기발광 소자는, 발광 효율이 높고, 화소 결함이 없고, 장수명인 유기 전기발광 소자 및 그것을 실현하는 다환계 화합물이다.

A kind of synthetic method of 9,10- neighbour's naphthyl anthracene -2,3,6,7- tetracarboxylic acid dianhydrides

本发明公开了一种9,10‑邻萘基蒽‑2,3,6,7‑四甲酸二酐的合成方法，具体包括如下步骤：(1)制备2,3,6,7‑四甲基‑9,10‑邻萘基蒽；(2)用2,3,6,7‑四甲基‑9,10‑邻萘基蒽合成9,10‑邻萘基蒽‑2,3,6,7‑四甲酸；(3)用9,10‑邻萘基蒽‑2,3,6,7‑四甲酸合成9,10‑邻萘基蒽‑2,3,6,7‑四甲酸二酐。本发明用两种不同的方法进行氧化均得到高价值的9,10‑邻萘基蒽‑2,3,6,7‑四甲酸损耗小，产率纯度均较高，易于大量生产。

A kind of Dihydrobenzofuranes C of 5 alkyl 2,360Fullerene double adduct and its production and use

本发明公开了一种5‑烷基‑2,3‑二氢苯并呋喃‑C 60 富勒烯双加成物及其制备方法和用途。如通式（I）所示的双加成物（其中R为甲基、乙基、异丙基、叔丁基或叔戊基）可以通过包括下列步骤的方法制备：1）制备对甲基苯磺酰亚胺碘苯；2）制备双加成中间体；和3）制备目标双加成物。本发明的双加成物合成温度低，反应时间短，易于分离纯化，有利于大规模生产；在可见光范围内具有良好的光吸收特性，适合于作为电子受体材料来构筑太阳能电池等光伏器件，极具科研开发和市场投资价值。

Selective oxabicycloalkanes

本发明涉及一类氧杂二环烷化合物及其在农业 上适用的组合物，以及在水稻作物位点施用有效量的 氧杂二环烷除草剂化合物来控制不希望有的植物生 长的方法。

Manufacture of 2,9-dioxatricyclo(4,3,1,o3,7) decane

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

METHOD FOR PRODUCING 7-OXABICYCLOHEPTANE COMPOUNDS AND NEW INTERMEDIATE PRODUCTS

(Poly-)Oxyalkylamino diphenyl ethers having herbicidal activity

Herbizid und den Pflanzenwuchs regulierende 3-(poly-)-Alkoxyamino-2'-chlor-4-nitro-4'-trifluormethyldiphenyläther der Formel I <IMAGE> worin A, A', A" und A‴ je ein gleicher oder verschiedender C1-C4-Alkylenrest der geradkettig oder verzweigt sein kann, n eine Zahl 1 bis 5 n',n", n‴ je Null oder eine Zahl von 1 bis 5 und R ein C1-C4-Alkylrest, ein C1-C4-Alkylcarbonylrest, wobei die Alkylreste durch Halogen oder Cyan substituiert sein können; ein Benzoyloder Phenylsulfonylrest der durch Halogen, C1-C4-Alkyl, C1-C4-Alkoxy, C1-C4-Halogenalkyl, C1-C4-Halogenalkoxy oder Nitro substituiert sein kann, oder falls A-O nicht Aethylenoxy und/oder falls die Summe von n, n', n" und n‴ grösser als 1 ist, auch Wasserstoff bedeuten, R1 Wasserstoff, C1-C4-Alkyl, C1-C4-Hydroxyalkyl, C2-C8-Alkoxyalkyl, C1-C4-Alkylcarbonyl oder C1-C4-Halogenalkylcarbonyl, wobei die Reste R und R1 über C-C oder C-O-Bindungen verzweigt oder gegebenenfalls auch miteinander ringgeschlossen sein können, und R2 Wasserstoff, Chlor oder Fluor bedeuten, eignen sich für die selektive Unkrautbekämpfung in Nutzpflanzenkulturen, wie Getreide, Mais, Reis oder Soja. Diese Wirstoffe wirken in kleineren Aufwandmengen als vergleichbare ähnliche bekannte Diphenyläther-Verbindungen. Daneben wirken diese Verbindungen gegen Insekten und Vertretern der Ordnung Akarina. Herbicide and plant growth regulating 3- (poly -) - alkoxyamino-2'-chloro-4-nitro-4'-trifluoromethyldiphenyl ether of the formula I <IMAGE> in which A, A ', A "and A ‴ are each the same or different C1 -C4-alkylene which can be straight-chain or branched, n is a number 1 to 5 n ', n ", n ‴ each zero or a number from 1 to 5 and R is a C1-C4-alkyl radical, a C1-C4-alkylcarbonyl radical, where the alkyl radicals can be substituted by halogen or cyano; a benzoyl or phenylsulfonyl radical which can be substituted by halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy or nitro, or ...

Method for preparing deoxyelephantolide or isodeoxyelephantolide

本发明公开了一种制备去氧地胆草内酯或异去氧地胆草内酯的方法。本发明提供的方法采用AB‑8大孔树脂初步富集和HSCCC分离纯化，可以制备得到纯度分别为99.6％、99.5％的去氧地胆草内酯、异去氧地胆草内酯，回收率分别达1.05g去氧地胆草内酯/1kg地胆草药材、2.38g异去氧地胆草内酯/1kg地胆草药材，纯度高且回收率高。

Functionalized bicyclic (meth) acrylates, process for their preparation and their use ####

7-oxabicyclo heptane carboxylic acid prostaglandin(PG) homologue intermediate and method for making thereof

本发明公开了制备下式结构的羧酸中间体的方 法，该羧酸中间体可用于制备最终的抗血栓形成和抗 血管痉挛的化合物。

Fused quinazoline derivatives useful as tyrosine kinase inhibitors

The present invention is directed to a compound having the structure wherein A is a 7–18 membered ring that comprises 0 to 6 heteroatoms selected from O, S, and N; R 1 is selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heterocyclyl; m is an integer from 0 to 3; X is selected from the group consisting of NR 2 , CHR 3 , O, or S; wherein R 2 and R 3 are each individually H or C 1-8 alkyl; R is selected from the group consisting of unsubstituted aryl, and substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl-(C 1-3 )alkyl, substituted or unsubstituted aryl-(C 3-7 )cycloalkyl, substituted or unsubstituted heteroaryl-(C 1-3 )alkyl, and substituted or unsubstituted heteroaryl-(C 3-7 )cycloalkyl; and pharmaceutically acceptable salts thereof; with the proviso that if A is a 7 or 8 membered ring, then R 1 is selected from the group consisting of other than H, C 1 –C 4 alkyl, (C 1 –C 4 alkoxy)C 1 –C 4 alkyl, C 1 –C 4 alkanoyl, C 1 –C 4 alkoxy or —S(O) x (C 1 –C 4 alkyl) wherein x is 0 to 2, and wherein said alkyl group and the alkyl moieties of said R 1 groups are optionally substituted by 1 to 3 halogens. The present invention is also directed to pharmaceutical compositions comprising the above compound, and methods of treating patients suffering from tyrosine kinase-mediated disorders using the above compound.

Lankacidin derivative and production thereof

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Hetero cyclic compound and organic light emitting device comprising the same

본 명세서는 화학식 1의 헤테로고리 화합물 및 이를 포함하는 유기 발광 소자에 관한 것이다. The present specification relates to a heterocyclic compound of Formula 1 and an organic light emitting device including the same.

Synthesis method of dicyclopentadiene dioxide

本发明公开了一种二氧化双环戊二烯的合成方法，是为了解决现有技术反应工艺复杂、选择性低和设备腐蚀严重的问题。本发明在相转移催化剂和磷钨酸催化下，以双环戊二烯为原料，过氧化氢为氧源合成了二氧化双环戊二烯，包括如下步骤：(1)将双环戊二烯和非质子溶剂加入反应瓶中，开启搅拌，加入磷钨酸和相转移催化剂；(2)开启加热，升至反应温度30～60℃，滴加质量分数30％的过氧化氢，反应4～9h；(3)冷却，过滤，有机层水洗至中性后无水硫酸钠干燥，蒸出溶剂得产品。本方法绿色环保，收率高，主要用于二氧化双环戊二烯的合成。

Small molecules and their use as organic semiconductors

The invention relates to novel compounds based on thieno[3,2-b]thiophene- 2,5-dione and/or furo[3,2-b]furan-2,5-dione or their thioketone derivatives, methods for their preparation and intermediates used therein, mixtures and formulations containing them, the use of the compounds, mixtures and formulations as semiconductor in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising these compounds, mixtures or formulations.

Functionalized bicyclic (meth) acrylates

Oxabicycloalkane derivatives,their preparation and their use as herbicides

PROCESS FOR THE PREPARATION OF INTERMEDIATES FOR USE IN THE PREPARATION OF 7-OXABICYCLOHEPTANE PROSTAGLANDINS

Halogen phenyl arylamine substituted norcantharidin, and preparation method and application thereof

本发明公开了一种卤苯基芳香胺取代去甲斑蝥素及其制备方法和应用，3’-卤苯基引入去甲斑蝥素衍生物结构中，形成3种去甲斑蝥酰胺酸衍生物：N-(3’-氯苯基)去甲斑蝥酰胺酸、N-(3’-溴苯基)去甲斑蝥酰胺酸和N-(3’-碘苯基)去甲斑蝥酰胺酸。此三种化合物具有广谱的抑制植物病原真菌的活性，可应用于斑蝥素类农用药剂的制备。

Small molecules and their use as organic semiconductors

本発明は、チエノ［３，２−ｂ］チオフェン−２，５−ジオンおよび／もしくはフロ［３，２−ｂ］フラン−２，５−ジオンに基づく新規な化合物またはそれらのチオケトン誘導体、それらの製造方法およびそれにおいて使用する中間体、それらを含む混合物および配合物、該化合物、混合物および配合物の有機電子（ＯＥ）デバイスにおける、特に有機光起電力（ＯＰＶ）デバイスおよび有機光検出器（ＯＰＤ）における半導体としての使用、ならびにこれらの化合物、混合物または配合物を含むＯＥ、ＯＰＶおよびＯＰＤデバイスに関する。

NOVEL POLYCYCLIC COMPOUNDS DERIVED FROM ANTHRACENE AND NAPHTHACENE AND PROCESS FOR THEIR PREPARATION

LA PRESENTE INVENTION CONCERNE DES COMPOSES DE FORMULE: (CF DESSIN DANS BOPI) OU R REPRESENTE UN METHYLE OU UN ALCOXY INFERIEUR, AINSI QUE DES PROCEDES POUR LEUR PREPARATION. THE PRESENT INVENTION RELATES TO COMPOUNDS OF FORMULA: (CF DRAWING IN BOPI) OR R REPRESENTS A LOWER METHYL OR ALCOXY, AS WELL AS PROCESSES FOR THEIR PREPARATION.

Patent FR2454433B1

CARBOXYMETHOXY-7 FURO- (3,4-C) -PYRIDINE MEDICINAL PRODUCTS

Lankacidin derivatives and production thereof

내용 없음.

Process for the preparation of synthetic ascaridol

New acyl-CoA: Cholesterol acyltransferase (ACAT) activity inhibitor and preparation method thereof

본 발명은 토양으로부터 분리된 곰팡이 아스퍼질러스 푸미가투스(Aspergillus fumigatus) FM-F-37로부터 분리된, 아실-CoA : 콜레스테롤 아실전이효소의 저해제인 하기 구조식(I)의 GERI-BP001, 그의 유도체 및 그의 제조방법에 관한 것이다.

Novel 1,4-bis-substituted-2,6,7-trioxabicyclo [2.2.2] octane pesticide

Exo-dicyclopentadiene dioxide

Halogenated heterocyclic ether herbicides

Formulations, salts, and solid forms of substituted cyclohexylmethanamines, processes for preparation, and uses thereof

Provided herein are pharmaceutical compositions and single unit dosage forms comprising a substituted cyclohexylmethanamine, or a pharmaceutically acceptable salt or solid form thereof. Also provided are methods of making the substituted cyclohexylmethanamine, or a pharmaceutically acceptable salt or solid form thereof, methods of making a pharmaceutical composition comprising the substituted cyclohexylmethanamine, or a pharmaceutically acceptable salt or solid form thereof, and method of their use for treating, managing, or preventing various disorders, such as a CNS disease.

2,6-dioxa-bicyclo-û2,2,2-octan-7-yl-acetaldehydes

2,6-Dioxabicyclo(2,2,2)octane derivs. of formula (I) are new. In (I), R1 = lower alkyl or benzyl; A and B = H or A+B = a bond.

Pharmaceutical composition of 7-oxabicycloheptane and 7-oxabicycloheptene compounds

Title compds. (I)[A,B=CH=CH, (CH2)2; m=1-8; X=OH, (a) CO2R1; R1=H, lower alkyl, etc.; Y=alkyl, alkenyl, cycloalkyl, thienyl, etc.; =single or double bond!, useful as a curing agent for cerebral thrombosis, were prepd.. Thus, 0.53mmol [1β, 2β (5Z), 3α (1E, 3S*), 4 β -7-[3-(3-cyclohexyl-3-hydroxy-1propenyl)-7-oxabicyclo [2,2,1 hept-2-yl -5-heptane (A) methyl ester was dissolved in 80% THF and treated with 1N Li(OH)2. After THF was evaporated, the resulting material was acidified with 10% oxalic acid, extd. with ether, concd., purified on CC7 silica gel, and filtered through polycarbonate membrane to give (A) (yield=86%).

Process for the manufacture of 2,9-dioxatricyclo(4,3,1,3 3'7)decanen

Halogenation II type polyketide compound, preparation method and applications

本发明公开了一种卤化II型聚酮类抗生素化合物，其特征在于，结构为： 本发明要解决的技术问题是提供一种较强的抗耐药金黄色葡萄球菌的卤化II型聚酮类抗生素化合物。

Biologically active product for controlling procreative metabolism

Process for preparing oxabicycloalkane compounds

Tetrathiafulvalene derivative precursors, tetrathiafulvalene derivatives, and processes for producing them

A tetrathiafulvalene derivative precursor represented by formula (1), a tetrathiafulvalene derivative represented by formula (6), and processes for producing the tetrathiafulvalene derivative precursor and the tetrathiafulvalene derivative: ##STR1## wherein R 1 and R 2 may be the same or different and represent organic groups that may be linked together to form a ring.

Be used to prepare 2- it is outer-method of (2- methylbenzyloxy) -1- methyl -4- isopropyl -7- oxabicyclo [2.2.1] heptane

本发明涉及一种制备式(I)的(±)‑2‑外‑(2‑甲基苄氧基)‑1‑甲基‑4‑异丙基‑7‑氧杂二环[2.2.1]庚烷、任何一种其单独对映体或其任何非外消旋混合物的方法，所述方法包括如下步骤：(a)使式(II)的(±)‑2‑外‑羟基‑1‑甲基‑4‑异丙基‑7‑氧杂二环[2.2.1]庚烷、任何一种其单独对映体或其任何非外消旋混合物在至少一种式[M m+ ] n [A n‑ ] m (III)的碱存在下脱质子化，其中M m+ 表示m价金属阳离子，其中m是1或2的整数，并且A n‑ 表示n价阴离子，其中n是1或2的整数，所述碱能够在反应条件下形成选自水、C 1 ‑C 4 烷基醇或其任意组合的溶剂S1，以形成式(IV)的金属醇盐或金属醇盐溶剂化物、任何一种其单独对映体或其任何非外消旋混合物，其中M m+ 、m和溶剂S1具有与对式(III)的碱定义相同的含义，并且x表示0‑10的数，和(b)使式(IV)的金属醇盐或金属醇盐溶剂化物、任何其单独对映体或其任何非外消旋混合物与式(V)的2‑甲基苄基化合物反应，其中X是离去基团，其中步骤(a)和(b)在至少一种惰性有机溶剂S2存在下进行，并包括(c)同时由反应混合物移除溶剂S1的另一步骤。

Bromo-norcantharidin ethyl gallate as well as preparation method and application thereof

本发明公开了一种溴代去甲斑蝥素单酸乙酯，即5,6-二溴去甲斑蝥素单酸乙酯，结构式为式I。本发明提供的一种溴代去甲斑蝥素单酸乙酯，即开环的5,6-二溴去甲斑蝥素单酸乙酯，经活性测试证明其具有很好的抗肝癌效果，可作为一种高效低毒的斑蝥素抗肿瘤药物。本发明的制备工艺选择性好，原料易得，成本低廉，合成路线简单，便于操作实施，并且合成所得产物毒性小，安全，得率高，纯度高。因而该工艺具有高效、便捷、低成本的特点。

Tertiary amine salts of 3,6-endoxohydro-orthophthalic acids and their use as aquaticherbicides

The invention comprises tertiary amine salts of 3,6-endoxohydro-orthophthalic acids, being the acid and neutral salts of the acids with one or more tertiary amines of formula R1R2NR3 where R1 is a C12-C18 aliphatic hydrocarbon group and R2 and R3 are C1-C4 alkyl groups The acids have less than three double bonds in the ring and may be the dihydro, tetrahydro (both isomers) or hexahydro acids. The acids may be substituted by chlorine, bromine, C1-C4 alkyl, C1-C4 alkoxy, aryl, aryloxy, nitro, cyano, or haloalkyl groups. The amine may be a dialkylcocoamine, soyaamine, tallowamine, stearylamine, laurylamine, myristylamine, oleylamine, or linoleylamine. Specification 692,262 is referred to.ALSO:Aquatic herbicidal compositions comprise the acid and neutral salts of 3,6-endoxohydroorthophthalic acids with one or more tertiary amines of formula R1R2NR3, where R1 is a C12-C18 aliphatic hydrocarbon group and R2 and R3 are C1-C4 alkyl groups together with a solid or liquid carrier. The liquid carrier is preferably water. If desired, a dispersant may also be added, e.g. isopropyl alcohol, diacetone alcohol or other alcohols and ketones. The solid carrier may be an inert absorbent granulated clay.