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.
专利号:US-7678938-B2 优先权日:2005-05-10 标题:Optical resolution of 3-carbamoylmethyl-5-methyl hexanoic acid 发明人:HEDVATI LILACH; DEE-NOOR ZIV; SINGER CLAUDE; PILARSKI GIDEON 权利人:TEVA PHARMA 摘要:The invention relates to pure (R)-CMH and to the optical resolution of CMH-racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)-CMH and to the process for isolating (S)-CMH from the mother liquor.