普瑞巴林的合成  

Synthesis of Pregabalin

作　　者：张桂森[1] 杨相平 刘笔锋[1] 

机构地区：[1]华中科技大学生命科学与技术学院,湖北武汉430072 [2]江苏恩华药业集团技术中心,江苏徐州221007

出　　处：《中国医药工业杂志》2007年第9期617-618,共2页Chinese Journal of Pharmaceuticals

摘　　要：异戊醛经Knoevenagel缩合、Michael加成、水解脱羧得3-异丁基戊二酸,与尿素酰亚胺化反应得3-异丁基戊二酰亚胺,再经Hofmann重排得3-(氨甲基)-5-甲基己酸,用(S)-(+)-扁桃酸拆分得普瑞巴林,总收率为33%。Pregabalin was synthesized with 33 % overall yield, from isovaleraldehyde by Knoevenagel condensation, Michael addition and hydrolysis to give 3-isobutylglutaric acid, which was subjected to imidization with urea followed by Hofmann rearrangement to afford 3-aminomethyl-5-methylhexanoic acid which was resolved with （S） mandelic acid.

关 键 词：普瑞巴林 抗癫痫药 止神经痛剂 合成 

分 类 号：TQ463.54[化学工程—制药化工]