4-氯-3-羟基丁腈 反应生成(S)-4-氯-3-羟基丁腈 参考文献:A Novel Generation Of Optically Active Ethyl 4-Chloro-3-Hydroxybutyrate As A C4 Chiral Building Unit Using Microbial Dechlorination 标题:A Novel Generation Of Optically Active Ethyl 4-Chloro-3-Hydroxybutyrate As A C4 Chiral Building Unit Using Microbial Dechlorination 摘要:A Novel Procedure For The Generation Of Optically Active Ethyl 4-Chloro-3-Hydroxybutyrate Using Bacterial Cells Was Developed. Ethyl (S)-4-Chloro-3-Hydroxybutyrate Was Prepared By Pseudomonas Sp. Os-K-29,Which Stereoselectively Assimilates 2,3-Dichloro-1-Propanol. The Reaction Was Based On Its Kinetic Dehalogenation For Both Enantiomers Using The Resting Cells. The Obtained 4-Chloro-3-Hydroxybutyrate Rate Had High Enantiomeric Excess Of >98%,With A Yield Of 33% At The Microbial Resolution Step. Moreover,Several C4 Compounds Having The 4-Chloro-3-Hydroxyl Function Were Also Resolved And Gave Good Enantiomeric Purities (>95 %ee). Ethyl (R)-4-Chloro-3-Hydroxybutyrate Was Also Obtained With High Enantiomeric Purity (>98 %ee) Using The Cells Of Pseudomonas Sp Ds-K-Nr818. Copyright (C) 1996 Elsevier Science Ltd Doi:10.1016/0957-4166(96)00410-7
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:WO-2025087822-A1 优先权日:2023-10-23 标 题 :New process for the preparation of (3r)-fluoropyrrolidine hydrochloride 发明人:ENGL PASCAL STEPHAN; HILDBRAND STEFAN; MOESSNER CHRISTIAN; STOECKLI MARKUS; STUTZ ALFRED 权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE 摘要:The present invention relates to a new process for the preparation of (3R)-3-fluoropyrrolidine hydrochloride or an acceptable salts thereof via a N-Boc-(3S)-3-hydroxypyrrolidine intermediate. The process is suitable for the synthesis of N-Boc-(3S)-3- hydroxypyrrolidine at technical scale in high, not less than 99.85%-a/a optical purity and a purity of not less than 99.8%-a/a. The high quality N-Boc-(3S)-3-hydroxypyrrolidine can be converted to (3R)-3-fluoropyrrolidine hydrochloride exhibiting an optical purity of not less than 99.95%-a/a and a purity of not less than 99.5%-a/a thus making it a suitable intermediate for manufacturing of pharmaceutical active compounds.
专利号:WO-2014203045-A1 优先权日:2013-06-20 标 题:A novel, green and cost effective process for synthesis of tert-butyl (3r,5s)-6-oxo-3,5-dihydroxy-3,5-o-isopropylidene-hexanoate 发明人:ROY BHAIRABNATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI ANURAG; PISE VIJAY SADASHIV; RUPANWAR MANOJ 权利人:LUPIN LTD 摘要:The present invention provides a process of preparation of an intermediate useful for the preparation of statins more particularly the present invention relates to an eco-friendly and cost effective process for the preparation of tert -butyl (3R,5S)-6-oxo-3,5-dihydroxy- 3,5-O-isopropylidene-hexanoate [I].
专利号:US-2002010339-A1 优先权日:1998-05-26 标 题:Method for synthesis of halopyridyl-acyclopentane derivative and intermediate thereof
专利号:US-9303001-B2 优先权日:2011-07-19 标 题 :Intermediate of statin drugs and preparation thereof 发明人:ZHANG SHOUHUA; WANG ZHONGQING; LUO ZHONGHUA 权利人:ZHANG SHOUHUA; WANG ZHONGQING; LUO ZHONGHUA; SUNSHINE LAKE PHARMA CO LTD; YICHANG HEC CHANGJIANG PHARMACEUTICAL CO LTD 摘要:The present invention relates to the field of pharmaceutical chemistry, specifically relates to a statin intermediate having formula I and preparation thereof. n nThe advantages of the method used to prepare the chiral sulfone intermediate having formula I are that a fluorophore is introduced at the beginning of the synthesis, and the intermediates are mostly solid, which enables quality control to be easily carried out.
专利号:KR-20050031140-A 优先权日:2003-09-29 标题 :A process for the synthesis of 3-hydroxy-γ-butyrolactone
参考文献:10.1007/s00253-024-13272-6 摘要:Martínková L, Kotik M, Kulik N, Křístková B, Šťastná K, Winkler M. Aldoxime dehydratases: production, immobilization, and use in multistep processes. Appl Microbiol Biotechnol. 2024 Nov 15;108(1):518.