原料药依帕司他的合成工艺优化研究
Study on the synthesis process of epalrestat
杨藏军1
作者信息
- 1. 河北冀衡药业股份有限公司,河北衡水 053400
- 折叠
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I 3-羧甲基若丹宁;以苯甲醛,丙醛为原料,经缩合反应得中间体Ⅲα-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.
Abstract
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 materials α-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Key words
epalrestat/3-carboxymethyl rhodanine/α-Methylcinnamaldehyde/glycine/condensation reaction引用本文复制引用
出版年
2024
国家科技期刊平台
NSTL
万方数据