原料药依帕司他的合成工艺优化研究  

Study on the synthesis process of epalrestat

作　　者：杨藏军 Yang Cangjun(Hebei Jiheng Pharmaceutical Corporation Ltd.,Hengshui 053400,China)

机构地区：[1]河北冀衡药业股份有限公司,河北衡水053400

出　　处：《煤炭与化工》2024年第4期145-148,共4页Coal and Chemical Industry

基　　金：河北省省级科技计划资助(199676234H)。

摘　　要：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.

关 键 词：依帕司他 3-羧甲基若丹宁 α-甲基肉桂醛 甘氨酸 缩合反应 

分 类 号：TQ469[化学工程—制药化工]