首页> 外国专利> PROCESS FOR THE PREPARATION OF SYN-ISOMER OF 2-(2-AMINOTHIAZOL-4-YL)-2-METHOXYIMINO ACETYL CHLORIDE HYDROCHLORIDE

PROCESS FOR THE PREPARATION OF SYN-ISOMER OF 2-(2-AMINOTHIAZOL-4-YL)-2-METHOXYIMINO ACETYL CHLORIDE HYDROCHLORIDE

机译:2-(2-氨基噻唑-4-基)-2-甲氧基亚氨基乙酰氯盐酸盐的合成异构体的制备方法

摘要

A process for the preparation of syn-isomer of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetyl chloride hydrochloride containing up to 5 wt.% of the anti-isomer of formula (III) by reacting the anhydrous acid hydrochloride salt of the syn-isomer of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid with a mixture containing at least one molar equivalent of oxalyl chloride and at least one molar equivalent to a slight excess of dimethylformamide to an amount of said oxalyl chloride in an inert organic solvent at a temperature of less than -10 DEG C. The compound is a useful intermediate for preparing broad spectrum antibacterial agents, cefepime dihydrochloride hydrate which is also known as 7-[2-(2- -aminothiazol-4-yl)-2-(Z)-methoxyiminoacetamido]-3-[(1- -methyl-1-pyrrolidinio)-methyl]ceph-3-em-4-carboxylate.
机译:通过使无水酸反应来制备2-(2-氨基噻唑-4-基)-2-甲氧基亚氨基乙酰氯盐酸盐的顺式异构体的方法,所述式(I)含有至多5重量%的式(III)的反式异构体2-(2-氨基噻唑-4-基)-2-甲氧基亚氨基乙酸的同分异构体的盐酸盐与含有至少一个摩尔当量的草酰氯和至少一个摩尔当量的二甲基甲酰胺的混合物低于-10℃的温度下,在惰性有机溶剂中加入一定量的上述草酰氯。该化合物是制备广谱抗菌剂头孢吡肟二盐酸盐水合物的有用中间体,也称为7- [2-(2 -氨基噻唑-4-基)-2-(Z)-甲氧基亚氨基乙酰胺基] -3-[(1-甲基-1-吡咯烷二基)-甲基] ceph-3-em-4-羧酸酯。

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