CAS: 148553-50-8; Pregabalin

上下游产品

CAS号181289-39-4 (3S)-3-Cyano-5-... | CAS号1078737-39-9 (S)-pregabalin-... | CAS号1310495-04-5 (S)-3-(aminomet... | CAS号128013-69-4 3-(氨甲基)-5-甲基己酸 | CAS号181289-33-8 (R)-(-)-3-(氨甲酰甲... | CAS号181289-37-2 (3S)-3-氰基-5-甲基己酸

(S)-5-Methyl-3-Cyanohexanoic Acid P-Chlorophenyl Ester置于乙醇,5%-Palladium/activated Carbon,氢气,Sodium Hydroxide体系中,用 乙醇 用作溶剂,25.0~40.0 °C,5.0 Mpa 条件下,反应 9.0H,反应生成普瑞巴林
参考文献:一种绿色高效的普瑞巴林合成方法
标题:一种绿色高效的普瑞巴林合成方法
摘要:本发明涉及一种绿色高效的普瑞巴林合成方法,包括:1)乙酸酯与异戊醛经脱水缩合得到5‑甲基‑2‑己烯酸酯;2)5‑甲基‑2‑己烯酸酯经氰基加成得到(S)‑5‑甲基‑3‑氰基己酸酯;3)(S)‑5‑甲基‑3‑氰基己酸酯经氢气还原成环得到(S)‑4‑异丁基吡咯烷‑2‑酮;4)(S)‑4‑异丁基吡咯烷‑2‑酮经水解开环得到普瑞巴林.该合成路线原料廉价易得,反应步骤少,工艺条件温和,操作简单,反应收率高,环境污染小,更加适合工业化生产原料药普瑞巴林.

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

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-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

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-7423169-B2
优先权日:2001-06-11
标 题:Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
发明人：RAILLARD STEPHEN P; ZHOU CINDY X; YAO FENMEI; MANTHATI SURESH KUMAR; XIANG JIA-NING; GALLOP MARK A
权利人:XENOPORT INC
摘要:The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.