头孢磺啶合成工艺的改进

Improved synthesis of Cefsulodin

目的改进头孢磺啶的合成工艺。方法以苯乙酸为原料,经磺化、拆分、酰化、酰胺化和取代五步反应合成头孢磺啶。结果与结论通过改进关键中间体7-(α-磺苯乙酰胺)-头孢菌素酸钠合成的投料比与后处理方法,使该步反应产率由30%提高到42%。

OBJECTIVE To improve the process of the synthesis of Cefsulodin. METHODS Cefsulodin was prepared, taking phenylacetic acid as the starting material, followed by sulfonation, resolution, acylation, amidation and substitution, in 5 steps totally. RESULTS and CONCLUSION The proportion of the ingredients and the method of the postprocessing had been improved in the process of synthesis of the key intermediate α - sulfobenzyl cephalosporin, with the increased yield from 30% to 42%.