头孢地嗪钠合成工艺改进

Synthesis of cefodizime sodium

目的优化头孢地嗪钠的合成工艺。方法 7-ACA与2-巯基-4-甲基-5-噻唑乙酸反应生成7-氨基-3-(5-羧甲基-4-甲基-1,3-噻唑-2-巯甲基)头孢-2-烯-2-羧酸,其与AE活性酯反应生成头孢地嗪酸,最后头孢地嗪酸与异辛酸钠反应成头孢地嗪钠。结果目标化合物结构经核磁共振氢谱确证,总收率可达63%。结论本文为头孢地嗪钠的工业化生产提供了一条较为合理的工艺路线。

Objective To improve the manufacturing process of cefodizime sodium.Method The reaction between 7-ACA and 2-mercapto-4-methyl-5-thiazolylacetic acid to give 7-amino-3-（5-（carboxymethyl-4-methyl-1,3-thiazolyl-2-yl-thiomethyl）-ceph-3-em-4-carboxylic acid,which was conducted with 2-（2-amino-thiazol-4-y1）-2-（Z）-methoxyiminoacetic acid S-benzthiazolyl thioester and sodium 2-ethylhexanoate to yield cefodizime sodium.Results The chemical structure of the target compound was confirmed by 1H-NMR.The total yield was 63%.Conclusion This article can provide a more reasonable operational route for the manufacturing process of cefodizime sodium.？