专利号:US-7230119-B2 优先权日:2004-08-25 标 题 :Process for the preparation of substituted pyrrolidine derivatives and intermediates 发明人:CHAND POORAN; EL-KATTAN YAHYA; KOTIAN PRAVIN L 权利人:BIOCRYST PHARM INC 摘要:Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.
专利号:US-6376683-B1 优先权日:2001-06-01 标 题:Process for the preparation of (4R,6S)-4-hydroxy-6-hydroxymethyl-tetrahydropyran-2-one 发明人:KUMAR PRADEEP; FERNANDES RODNEY AGUSTINHO 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to an improved, efficient and enantio-selective process for the synthesis of (4R, 6S)-4-hydroxy-6-hydroxymethyl tetrahydropyran-2-one, employing the Sharpless asymmetric dihydroxylation and regiospecific nucleophilic hydride opening of the cyclic sulfite/sulfate as the key steps. The invention also resides in the intermediates used in the process.
专利号:US-8354530-B2 优先权日:2005-07-28 标 题:Process for the synthesis of rosuvastatin calcium 发明人:ZLICAR MARKO 权利人:LEK PHARMACEUTICALS; ZLICAR MARKO 摘要:Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.
专利号:US-2023339839-A1 优先权日:2022-04-24 标题:Synthesis method of alpha-hydroxycarboxylic acid ester 发明人:MENG ZHONGLEI; QIN RONGXIU; GAO SHOUNA; HU GUOJIAO; WEN RUSI; Liao Zhongqiu; LIANG ZHONGYUN; HU LIHONG; ZHOU YONGHONG 权利人:GUANGXI FORESTRY RES INSTITUTE 摘要:A synthesis method of alpha-hydroxycarboxylic acid ester is provided. In the method, an alpha-hydroxycarboxylic acid and an alcohol are taken as raw materials, one or more of boric acid, metaboric acid, pyroboric acid, and boric anhydride is taken as a catalyst, and one of cyclohexane, toluene, benzene, and alcohols is taken as a water-carrying agent. A reaction temperature is kept in range of 100-160° C., produced water is separated by an oil-water separator, and the alpha-hydroxycarboxylic acid ester is synthesized directly. After an esterification reaction, the water-carrying agent and unreacted alcohol are distilled by vacuum fractionation to obtain a crude product, and refined alpha-hydroxycarboxylic acid ester is obtained by performing neutralization, water washing, and vacuum rectification on the crude product. The alpha-hydroxycarboxylic acid ester prepared by the method has high purity and light color, and can be used as green solvent, surfactant, chiral resolution agent and plasticizer.
专利号:WO-2011088425-A2 优先权日:2010-01-15 标题 :Electro-autotrophic synthesis of higher alcohols
专利号:WO-9000611-A1 优先权日:1988-07-15 标题 :Synthesis of stereospecific enzyme by non-chromosomal transformation of a host
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