Class / Patent application number | Description | Number of patent applications / Date published |
544315000 | At 2-position | 58 |
20100063282 | Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions, and Uses Thereof - Compounds of Formula (I) | 03-11-2010 |
20110178297 | Process for the synthesis of halogenated cyclic compounds - A process for the manufacture of a cyclic compound of formula (I) | 07-21-2011 |
20150360066 | USE OF METAL-ACCUMULATING PLANTS FOR IMPLEMENTING CHEMICAL REACTIONS - A method of implementing organic synthesis reactions uses a composition containing a metal catalyst originating from a calcined plant. The plants can be from the Brassicaceae, Sapotaceae and Convolvulaceae family, and the metal catalyst contains metal in the M(II) form such as zinc, nickel, manganese, lead, cadmium, calcium, magnesium or copper. Examples of the organic synthesis reactions include halogenations, electrophilic reactions, cycloadditions, transesterification reactions and coupling reactions, among others. | 12-17-2015 |
544316000 | Nitrogen attached directly or indirectly to the diazine ring by nonionic bonding | 49 |
20100105904 | UREA TYPE CINNAMIDE DERIVATIVE - Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. | 04-29-2010 |
20100174076 | COUMARIN DERIVATIVES USEFUL AS TNF ALPHA INHIBITORS - Novel compounds composition capable of inhibiting TNFα and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds. | 07-08-2010 |
20100197917 | COUMARIN DERIVATIVES USEFUL AS TNF ALPHA INHIBITORS - Novel compounds composition capable of inhibiting TNFα and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds. | 08-05-2010 |
20100317855 | PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE (2S,3S,5S)-5-AMINO-2-N,N-DIBENZYLAMINO-3-HYDROXY-1,6-DIPHENYLHEXANE - The present invention relates to the purification of (2S,3S,5S)-5-amino-2-N,N-dibenzylamino-3-hydroxy-1,6-diphenylhexane (III) by making its crystalline acid addition salt, which can be used as such to produce Lopinavir/Ritonavir with high purity and yield. Formula III | 12-16-2010 |
20100324289 | Chemical Process - The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR | 12-23-2010 |
20110071290 | Process And Catalyst - Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents. | 03-24-2011 |
20110144333 | 4,5-DIHYDRO-OXAZOL-2YL DERIVATIVES - The invention relates to compounds of formula I | 06-16-2011 |
20110178298 | REDUCTION OF 5-(ARYL-DIAZENYL)-4,6-DIHALO-PYRIMIDINE - Method of synthesizing a compound of formula (I), wherein R1, R2 are, independently, chloro or fluoro, and wherein R3 is H, alkyl, aralkyl or is an alkylether or alkylthioether comprising the steps of firstly reducing a diazeny compound of formula (II) non-catalytically or with a catalytic amount of an homogenous organic, non-metal catalyst to the corresponding hydrazo compound of formula (III) and in a second step catalytically hydrogenating said hydrazo compound in with a heterogeneous Ni-catalyst to the compound of formula (I). | 07-21-2011 |
20110224435 | PROCESS FOR PREPARATION OF AMORPHOUS LOPINAVIR - The present invention relates to a process for preparation of amorphous lopinavir, which is HIV protease inhibitor of Formula (I). Using agitated film drying. | 09-15-2011 |
20110251388 | 1-HETERODIENE DERIVATIVE AND HARMFUL ORGANISM CONTROL AGENT - The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R | 10-13-2011 |
20110275812 | PROCESS FOR THE PREPARATION AND PURIFICATION OF ETRAVIRINE AND INTERMEDIATES THEREOF - In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. The compound, 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile “ETHER” of formula (A) wherein n is either 0 or 1 and HA is an acid. | 11-10-2011 |
20120172596 | REGIOSELECTIVE PREPARATION OF 2-AMINO-5-TRIFLUOROMETHYLPYRIMIDINE DERIVATIVES - The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula T-H; and reacting the compound obtained with an amine of formula (II) [HN(R1)R2] to form a compound of formula (III) wherein X1, X2, T, R1 and R2 have the meanings as defined herein. | 07-05-2012 |
20130035485 | PROCESS FOR THE PREPARATION AND PURIFICATION OF ETRAVIRINE AND INTERMEDIATES THEREOF - In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. | 02-07-2013 |
20130245260 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula: | 09-19-2013 |
20140213786 | Method for Producing Coumarin Derivative - The present invention provides a novel method for producing a compound represented by general formula (VII) below or a pharmaceutically acceptable salt thereof or a synthetic intermediate thereof: | 07-31-2014 |
20140303369 | Crystalline Pharmaceutical - New crystalline forms of lopinavir are disclosed. | 10-09-2014 |
20160251340 | HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS | 09-01-2016 |
544317000 | The nitrogen is bonded directly at 4- or 6-position | 32 |
20080214811 | XANTHENE DYES - The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates. | 09-04-2008 |
20080214812 | Trisubstituted triazolopyrimidines for use in platelet aggregation inhibition - The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. | 09-04-2008 |
20090036679 | METHOD FOR RESOLVING ENANTIOMERS FROM RACEMIC MIXTURE HAVING CHIRAL CARBON IN ALPHA POSITION OF NITROGEN - Disclosed relates to a simplified method for resolving enantiomers by dissolving a racemic mixture having chiral carbon in α-position of nitrogen and an amino acid to prepare a diastereomeric salt, not using catalyses or enzymes, with enhancing the optical purity remarkably. Moreover, the present invention can prepare the enantiomers in large quantities without using expensive catalysts or without controlling the reaction conditions for the activity of enzymes applied. | 02-05-2009 |
20090105478 | NOVEL COMPOUNDS - Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. | 04-23-2009 |
20090192310 | Process and Intermediates for Preparing Emtricitabine - A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described. | 07-30-2009 |
20090198056 | Beta secretase inhibitor - The present invention relates to a compound of the formula (1): | 08-06-2009 |
20090306380 | Process for preparing 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde - Provided are a process for preparing a 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde, which is industrially advantageous in that a 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde can be prepared in high yield in a simple way, an intermediate used in the process, and a process for preparing the intermediate, which is industrially advantageous in that the intermediate can be prepared safely in high yield with ease. | 12-10-2009 |
20100063283 | PROCESS FOR STEREOSELECTIVE SYNTHESIS OF LAMIVUDINE - A process for stereoselective synthesis of lamivudine, comprising (a) glycosylation of compounds of formula (I) and cytosine or protected cytosine, separating the resulting products by crystallization to afford intermediates of formula (II); (b) removing the protecting groups of intermediates of formula (II) to obtain lamivudine. | 03-11-2010 |
20100184979 | NEW PROCESS FOR PREPARING 2-(3--PHENYL)-2-METHYLPROPRIONIC ACID - This invention is directed to a process for preparing 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid. | 07-22-2010 |
20100190982 | PROCESS FOR THE PREPARATION OF LAMIVUDINE FORM I - The present invention provides a process for preparing a stable crystalline solid of Lamivudine polymorphic Form I, which does not change to Form II during storage and pharmaceutical unit operations. | 07-29-2010 |
20100286393 | Increasing the In Vivo Biological Activity of Biologically Active Compounds - The present invention relates to compounds with an increased in vivo biological activity, and especially an increased pharmaceutical activity, such as an anti-nematodal or antifungal activity, an immunosuppresive activity, a metabolism influencing activity and/or an anti-cancer activity. Specifically, the present invention relates to compound comprising an artemisinin derivative according to the general formula (I) | 11-11-2010 |
20100305320 | Polymorph, polymorph screening system, and polymorph preparing and screening method - A polymorph, a polymorph screening system, and a polymorph preparing and screening method are disclosed. The polymorph preparing and screening method includes the following steps: providing a plurality of substrates of different materials; causing an organic material to grow crystals on the plurality of substrates through solution-cooling crystallization process, so that a plurality of polymorphs with different characteristics are prepared; and screening the plurality of polymorphs prepared in the previous step to obtain polymorphs with desired characteristics. | 12-02-2010 |
20100305321 | PROCESS FOR CHIRAL RESOLUTION OF 2-SUBSTITUTED 4-SUBSTITUTED 1,3-OXATHIOLANES - The present invention relates to a novel process for the chiral resolution of 2-substituted 4-substituted 1,3-oxathiolanes and derivatives thereof. The present invention also relates to novel 2-substituted 4-substituted 1,3-oxathiolanes derivatives. | 12-02-2010 |
20100324290 | CRYSTALLINE FORM I OF LAMIVUDINE AND ITS PREPARATION - The present invention relates to a stable crystalline Form I of lamivudine. The present invention further relates to a process for the preparation of the stable crystalline Form (I) of the stable crystalline Form (I) of lamivudine. | 12-23-2010 |
20110112294 | 1-[2', 3' -DIDEOXY-3' C- (HYDROXYMETHYL) - BETA-D-ERYTHRO-PENTOFURANOSYL] CYTOSINE DERIVATIVES AS HIV INHIBITORS - Compounds of the formula I | 05-12-2011 |
20110137034 | PROCESS FOR PREPARING LAMIVUDINE POLYMORPH FORM - The invention relates to a process for the preparation of stable lamivudine polymorph form and to a composition comprising thereof. | 06-09-2011 |
20110213148 | Co-crystal compound of optical device - The present invention discloses a co-crystal compound of optical devices. The co-crystal compound is crystallized out with hydrogen bonding by a temperature fluctuation method after mixing small organic molecules without optoelectronic properties and organic molecules having heterocyclic rings with optoelectronic properties. The photoluminescence (PL) intensity of this hydrogen-bonded co-crystal compound according to the present invention can vary with a variety of the small organic molecules without optoelectronic properties, so as to modulate the PL intensity. | 09-01-2011 |
20110245497 | OPTICAL RESOLUTION OF SUBSTITUTED 1, 3-OXATHIOLANE NUCLEOSIDES - Cis(±)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone is reacted with S(+)-1,1′-binaphthyl-2,2′-diyl hydrogen phosphate in methanol to obtain diastereomeric compounds. The diastereomeric compounds are subjected to selective crystallization to obtain (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1′-binaphthyl-2,2′-diyl hydrogen phosphate. (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1′-binaphthyl-2,2′-diyl hydrogen phosphate is treated with hydrochloric acid in water to obtain (2R-cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone. | 10-06-2011 |
20110257396 | PROCESS FOR THE MANUFACTURE OF CIS(-)-LAMIVUDINE - An improved process for the manufacture of Lamivudine. The process involves: | 10-20-2011 |
20110257397 | Process and methods for the preparation of optically active cis-2-hydroxymethyl-4-(cytosin-1'-yl)-1,3-oxathiolane or pharmaceutically acceptable salts thereof - There is provided a method for resolving a compound of formula III, in the cis configuration: | 10-20-2011 |
20110288298 | NOVEL POLYMORPH OF EMTRICITABINE AND A PROCESS FOR PREPARING OF THE SAME - A polymorph of emtricitabine, wherein said polymorph displays angular positions of characteristic peaks in powder X-ray diffraction pattern 13.61±0.2, 15.54±0.2, 19.49±0.2, 20.55±0.2, 25.89±0.2, 28.09±0.2 and 29.10±0.2. A pharmaceutical composition comprising a polymorph of emtricitabine displaying angular positions of characteristic peaks in powder X-ray diffraction pattern 13.61±0.2, 15.54±0.2, 19.49±0.2, 20.55±0.2, 25.89±0.2, 28.09±0.2 and 29.10±0.2. A process for the preparation of a polymorph of emtricitabine comprising the steps of (a) dissolving crude emtricitabine in polar organic solvent by heating at a temperature of at least 40° C. and not more than 150° C. to form a reaction mixture optionally decreasing the concentration of polar organic solvent in said reaction mixture; cooling the reaction mixture obtained in step (a); and separating the solid from the cooled reaction mixture resulted in step (b). | 11-24-2011 |
20120184739 | ENANTIOMERIC RESOLUTION OF 2,4-DISUBSTITUTED 1,3-OXATHIOLANE NUCLEOSIDES - Single enantionmers of compounds of formula (B), in either the cis or trans configuration, | 07-19-2012 |
20120316339 | Preparation of Lamivudine Form I - A thermodynamically controlled process for preparing Form I polymorph of lamivudine is described, wherein the process involves crystallizing Form I at a temperature of from about 0° C. to about 50° C. from a mixture which comprises (a) lamivudine or an acid salt thereof or both, (b) a solvent system comprising water and at least one organic solvent, and optionally (c) Form I seed; wherein, when a lamivudine acid salt is employed in the mixture, the crystallizing step is conducted in the presence of a base; and wherein the water activity of the solvent system is maintained in a range in which Form I is thermodynamically the most stable form of lamivudine. | 12-13-2012 |
20130053560 | LAMIVUDINE OXALATE AND PREPARATION METHOD THEREOF - Lamivudine oxalate, preparation method and crystalline forms thereof are disclosed. A preparation method of Lamivudine is also disclosed. | 02-28-2013 |
20130072681 | PROCESS FOR STEREOSELECTIVE SYNTHESIS OF 5-FLUORO-1-(2R,5S)-[2-(HYDROXYMETHYL)-1,3-OXATHIOLAN-5-YL]CYTOSINE - The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof. | 03-21-2013 |
20130296562 | STEREOSELECTIVE PROCESS FOR PREPARATION OF 1,3-OXATHIOLANE NUCLEOSIDES - The present invention relates to a stereoselective glycosylation for the preparation of 1,3-oxathiolane nucleoside in high yield and high optical purity. The invention specifically relates to a process of the preparation of Lamivudine and Emtricitabine using zirconium (IV) chloride (ZrCl | 11-07-2013 |
20140046062 | PROCESS FOR NUCLEOSIDES - The present invention relates to improved process for the preparation of lamivudine or emtricitabine. Thus, (1′R,2′S,5′R)-menthyl-5(R,S)-acetoxy-[1,3]-oxathiolane-2(R)-carboxylate is reacted with N-propinoyl cytosine in hexamethyl disilazane and then added trityl perchlorate to obtain a solid containing (1′R,2′S,5′R)-menthyl-5S-(N-4″-propionylcytosin-1″-yl)-[1,3]-oxathiolane-2R-carboxylate. The solid obtained above is reacted with methane sulfonic acid to obtain (2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-[1,3]-oxathiolane-2-carboxylic acid, 2S-isopropyl-5R-methyl-1R-cyclohexyl ester. The above compound is reduced with sodium borohydride to obtain lamivudine. | 02-13-2014 |
20140187777 | MATERIALS AND METHODS FOR THE BASE-ASSISTED SYNTHESIS OF SUBSTITUTED HETEROAROMATIC COMPOUNDS - Disclosed herein are some methods for synthesizing the base-assisted coupling of aromatic alcohols with substituted aromatic compounds including some substituted heteroaromatic compounds such as pyrimidines or pyridines to form esters. The reactions may include inexpensive bases such as potassium hydroxide and take place in a solvent mixture comprised primarily of hindered tertiary alcohols that are at least partially immiscible with water. In some embodiments the tertiary alcohol solvents forms azeotropes with water which stabilize the formation of an alkoxide intermediate when the alkoxide formation step is heated to the boiling point of the azeotrope and water is withdrawn from the reaction mixture. | 07-03-2014 |
20140275536 | NOVEL PHENOL DERIVATIVES AND PHARMACEUTICAL OR COSMETIC USE THEREOF - The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): | 09-18-2014 |
20140275537 | PROCESS FOR THE PREPARATION OF 4-AMINO-1-((1S,4R,5S)-2-FLUORO-4,5-DIHYDROXY-3-HYDROXYMETHYL-CYCLOPENT-2-- ENYL)-1H-PYRIMIDIN-2-ONE - Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described. | 09-18-2014 |
20150376142 | Process for the Preparation of 4-Amino-1-((1S,4R,5S)-2-Fluoro-4,5-Dihydroxy-3-Hydroxymethyl-Cyclopent-2-- Enyl)-1H-Pyrimidin-2-One - Processes for the preparation of 4-amino-1((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described. | 12-31-2015 |
20160024132 | SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO- -D-ARABINOFURANOSYL) CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME - A compound represented by a formula [1D] as shown below (wherein R | 01-28-2016 |
544318000 | Additional chalcogen attached directly or indirectly to the diazine ring by nonionic bonding | 6 |
20100121059 | 5-PHENOXYALKOXYPSORALENS AND METHODS FOR SELECTIVE INHIBITION OF THE VOLTAGE GATED Kv1.3 POTASSIUM CHANNEL - Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels). | 05-13-2010 |
20110160455 | Preparation of Aminopyrimidine Compounds - A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide. | 06-30-2011 |
20120277432 | Preparation of Aminopyrimidine Compounds - A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide. | 11-01-2012 |
20120316340 | USE OF METAL-ACCUMULATING PLANTS FOR THE PREPARATION OF CATALYSTS THAT CAN BE USED IN CHEMICAL REACTIONS - The use of metal-accumulating plants for implementing chemical reactions. | 12-13-2012 |
20130060031 | PROCESS FOR THE PREPARATION OF HIGHLY PURE AMBRISENTAN - The present invention relates to an improved and novel process for the preparation of highly pure (>99.8%) (+)-2(S)-(4,6-dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid (Ambrisentan) of formula (I). | 03-07-2013 |
20140249309 | Method for Preparing Optically Pure (+)-Ambrisentan and (+)-Darusentan - Disclosed is a method for preparing optically pure (+)-ambrisentan and (+)-darusentan, comprising: firstly catalyzing the asymmetric epoxidation of a β-unsaturated alkene using a chiral ketone derived from fructose or a hydrate thereof as a catalyst, and then subjecting the product to an epoxy compound ring-opening reaction and substitution reaction successively to obtain optically pure (+)-ambrisentan and (+)-darusentan. | 09-04-2014 |