普瑞巴林的绿色合成工艺  

Green Synthesis of Pregbalin

作　　者：张蔓[1] 刘怡忻[1] 

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《浙江化工》2013年第10期7-9,共3页Zhejiang Chemical Industry

摘　　要：以糠醛为起始原料,经Baeyer-Villiger反应,Michael加成反应,开环反应,最后再脱去保护基合成普瑞巴林。该路线的创新点是:(1)Baeyer-Villiger氧化反应,采用H2O2/HCOOH的氧化体系;(2)Michael加成反应,以CuI与含磷手性配体形成的络合物作为催化剂。这条新的合成路线原料廉价、手性配体相对简单、易得,绿色环保。Starting from furfural, pregbalin was synthesized through Baeyer-Villiger reaction, Michael addition reaction, ring cleavage reaction and deprotection reaction. The innovations of the route are as follows： （1） Baeyer-Villiger reaction by H202/HCOOH as the oxidation system; （2）Michael addition reaction by the complex （CuI with the chiral ligand containing P atom） as the catalyst. The new route has the advantages of cheap starting material, simple and available chiral ligand and lower cost with environmental friendly.

关 键 词：普瑞巴林 糠醛 合成 

分 类 号：TQ463[化学工程—制药化工]