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-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-2009081801-A1 优先权日:2007-08-15 标题:Process for synthesis of pyrrole derivative, an intermediate for atorvastatin 发明人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; PATEL HITESH K; RAO V GOVARDHAN; DAUND VAIBHAV S 权利人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; PATEL HITESH K; RAO V GOVARDHAN; DAUND VAIBHAV S 摘要:The present invention also relates to a novel impurity, (6-{2-[2-(6-{2-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-phenylcarbamoyl-pyrrol-1-yl]-ethyl}-2,2-dimethyl-[1,3]-dioxan-4-yl)-acetylamino]-ethyl}-2,2-dimethyl-[1,3]-dioxan-4-yl)-acetic acid tert-butyl ester, the compound of formula IV, having the following structure: n n n n n n n n n n The present invention also provides methods of preparing the compound of formula IV as well as methods of using the compound of formula IV as a reference marker and a reference standard. n The present invention also provides an improved process for preparing (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester, the compound of formula I, said process comprising the step of condensing 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzene butanamide, the compound of formula III, with (4R,Cis)-1,1-dimethylethyl-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxane-4-acetate, the compound of formula II, in the presence of a catalytic amount of an acid in the presence of a solvent system, preferably a binary solvent system, to obtain the desired compound (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester.
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.
参考标题:Chemo- And Regioselective Synthesis Of Acyl-Cyclohexenes By A Tandem Acceptorless Dehydrogenation-[1,5]-Hydride Shift Cascade 作者:Lewis B. Smith,Roly J. Armstrong,Daniel Matheau-Raven,Timothy J. Donohoe |发布日期:2020.2.5 摘要:Acceptorless Dehydrogenation Of The Diol Followed By A Redox-Neutral Cascade Process, Which Is Independent Of The Iridium Catalyst. Deuterium Labeling Studies Established That The Key Step Of This Cascade Involves A Novel Base-Mediated [1,5]-Hydride Shift. The Cyclohexenyl Ketone Products Could Readily Be Cleaved Under Mildly Acidic Conditions To Access A Range Of Valuable Substituted Cyclohexene Derivatives