头孢克肟的合成工艺研究

Study on the synthesis of cefixime

目的优化头孢克肟的合成工艺。方法以7-氨基-3-乙烯基头孢烷酸与2-(2-氨基-4-噻唑)-2-[[(z)-(叔丁氧羰基)甲氧]亚氨]-乙酸苯并噻唑硫酯为起始原料经酰胺化、水解反应得目标化合物。结果目标化合物经红外光谱和核磁共振氢谱确证化学结构,总收率80%,纯度99.2%。结论该制备过程操作简单,收率高,易于实现工业化。

Objective To improve the manufacturing process of cefixime. Methods Cefixime was synthesized by reaction of 7-amino-3-vinyl-3-cephem-4-carboxylic acid with 2-（2-aminothiazol-4-yl）-2-[[（Z）- （tert-butoxy Carbonyl）methoxy]imino] acetic acid-2- S-mercap to benzothiazole ester via amidation and hydrolysis. Results The chemical structure of the target compound was cofirmed by IR and ^1H-NMR. The total yield was 80%, and purity was 99.2%（HPLC）. Conclusion A more reasonable operational path for the manufacturing process of cefixime was provided by this expriment.