(+)-5-氨基-3-(S)-异丁基戊二酸置于对甲苯磺酸,Sodium Hydroxide,盐酸体系中,用 甲苯,水 用作溶剂,化学反应 1.5H,反应生成3-(氨甲酰甲基)-5-甲基己酸 参考文献: Process For Preparing Pregabalin And Its Intermediate[fr] Procédé De Préparation De La Prégabaline Et De Son Intermédiaire 标题: Process For Preparing Pregabalin And Its Intermediate[fr] Procédé De Préparation De La Prégabaline Et De Son Intermédiaire 摘要:提供了制备普瑞巴林及其中间体(如3-(氨甲酰)-5-甲基己酸)的工艺.制备普瑞巴林的过程主要包括将3-(氨甲酰)-5-甲基己酸与(+)-苯乙胺反应,然后在碱存在下与溴反应以获得普瑞巴林.
专利号:US-2007259917-A1 优先权日:2006-04-24 标题 :Processes for the synthesis of 3-isobutylglutaric acid 发明人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 权利人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 摘要:Provided are processes for the synthesis of 3-isobutylglutaric acid, an intermediate in the synthesis of (S)-Pregabalin.
专利号:US-8476441-B2 优先权日:2009-01-29 标 题 :Intermediates in the enantioselective synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid 发明人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN 权利人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN; TRINITY COLLEGE DUBLIN 摘要:(S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration.
专利号:US-2010087525-A1 优先权日:2008-06-23 标 题:Stereoselective enzymatic synthesis of (s) or (r)-iso-butyl-glutaric ester 发明人:HEDVATI LILACH; STERIMBAUM GRETA; RAIZI YURIY; AMINOV RAHAMIN 权利人:HEDVATI LILACH; STERIMBAUM GRETA; RAIZI YURIY; AMINOV RAHAMIN 摘要:The present invention relates to a stereoselective enzymatic synthesis of (S) or (R)-iso-butyl-glutaric ester, an intermediate of S-Pregabalin.
专利号:US-8212071-B2 优先权日:2005-09-19 标题:Asymmetric synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid 发明人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; RAO V GOVARDHAN; TIWARI ANAND PRAKASH 权利人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; RAO V GOVARDHAN; TIWARI ANAND PRAKASH; TEVA PHARMA 摘要:The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.
专利号:US-7462738-B2 优先权日:2006-05-24 标题:Processes for the preparation of R-(+)-3-(carbamoyl methyl)-5-methylhexanoic acid and salts thereof 发明人:HEDVATI LILACH; GILBOA EYAL; AVHAR-MAYDAN SHARON 权利人:TEVA PHARMA 摘要:Provided are processes for the synthesis of R-(+)-3-(carbamoylmethyl)-5-methylhexanoic acid and salts thereof, intermediates in the synthesis of S-pregabalin.
专利号:US-8168828-B2 优先权日:2007-06-25 标题 :Process for the preparation of pregabalin 发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU 权利人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU; MSN LAB LTD 摘要:The present invention encompasses novel intermediates of pregabalin, namely 3-cyano-5-methyl hexanamide (28) and 3-(amino methyl)-5 methyl hexanamide (29), and processes for their preparation. The invention also encompasses a process for converting the novel pregabalin intermediates into pregabalin, Formula (I): The present invention further provides a cost effective method for the synthesis of (S)-pregabalin, which involves the recovery of mandelic acid and tartaric acid used in the resolution process and recycling them, increasing the yields of the final product formed, which substantially reduced the cost of the production.
参考文献:10.1007/s13738-019-01759-3 摘要:Mansoori A, Zahednezhad F, Bavili Tabrizi A, Shahbazi Mojarrad J. Development of a new synthesis approach for S-pregabalin by optimizing the preparation stages. Journal of the Iranian Chemical Society. 2019 Aug 31;17(1):89–101. doi: 10.1007/s13738-019-01759-3.