2-(3-甲基丁亚基)丙二酸二乙酯置于氢溴酸,二正丙胺,乙酰氯体系中,用 水 用作溶剂,化学反应 91.08H,反应生成3-异丁基戊二酸酐 参考文献: Process For The Preparation Of R-(-)-3-(Carbamoylmethyl)-5-Methylhexanoic Acid And The Intermediates[fr] Méthode De Préparation D'Acide R-(-)-3-(Carbamoylméthyl)-5-Méthylhexanoïque Et De Ses Intermédiaires 标题: Process For The Preparation Of R-(-)-3-(Carbamoylmethyl)-5-Methylhexanoic Acid And The Intermediates[fr] Méthode De Préparation D'Acide R-(-)-3-(Carbamoylméthyl)-5-Méthylhexanoïque Et De Ses Intermédiaires
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-8063244-B2 优先权日:2009-05-07 标 题 :Process for the synthesis of pregabalin 发明人:RAZZETTI GABRIELE; ALLEGRINI PIETRO; PASTORELLO DARIO 权利人:RAZZETTI GABRIELE; ALLEGRINI PIETRO; PASTORELLO DARIO; DIPHARMA FRANCIS SRL 摘要:A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2  (III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.