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原料药依帕司他的合成工艺优化研究

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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.
Study on the synthesis process of epalrestat
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.

epalrestat3-carboxymethyl rhodanineα-Methylcinnamaldehydeglycinecondensation reaction

杨藏军

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河北冀衡药业股份有限公司,河北衡水 053400

依帕司他 3-羧甲基若丹宁 α-甲基肉桂醛 甘氨酸 缩合反应

2024

煤炭与化工
河北省化学工业研究院

煤炭与化工

影响因子:0.246
ISSN:2095-5979
年,卷(期):2024.47(4)