原料药依帕司他的合成工艺优化研究

Study on the synthesis process of epalrestat

提供了一种原料药依帕司他的合成方法,以甘氨酸为起始原料,经加成反应、取代反应、环合反应制得中间体Ⅰ3-羧甲基若丹宁;以苯甲醛,丙醛为原料,经缩合反应得中间体Ⅱα-甲基肉桂醛;中间体Ⅰ与中间体Ⅱ再经缩合反应,得依帕司他粗品,精制得成品。总收率60%以上,纯度99.24%,符合相关质量标准要求,该合成工艺路线简单,操作方便后处理简单,适合工业化生产。

A synthetic method for the active pharmaceutical ingredient iprastam,which uses glycine as the starting material and undergoes addition,substitution,and cyclization reactions to obtain the intermediate I3-carboxymethyl rhodanine were provided.Intermediate II was obtained through condensation reaction using benzaldehyde and propanal as raw materialsα-Methylcinnamaldehyde.Intermediate I and intermediate II undergo a condensation reaction to obtain crude iparameta and refined into finished products.The total yield of the product in the entire process is over 60%,with a purity of up to 99.24%,which meets the relevant quality standards.This synthesis process has a simple route,convenient operation,simple post-treatment,and is suitable for industrial production.