摘要
目的改进头孢他啶的生产工艺。方法以7-氨基头孢烷酸为起始原料、六甲基二硅胺烷为硅烷基化试剂,采用惰性气体排氨及新的除杂技术,经3位取代反应、7位酰化反应制备头孢他啶五水合物,最终得到目标产物头孢他啶。结果与结论目标产物的结构经IR1、H-NMR、13C-NMR谱数据确证。改进后的合成路线工艺稳定,操作简单,有利于工业化生产,产品流动性好,生产成本低廉,与原工艺相比总收率提高约10%。
Aim To improve the synthesis of ceftazidine.Methods Ceftazidine was synthesized from 7-aminocephalosporanic acid（7-ACA） firstly by 3-substitution then by 7-acylation.The new method of preparing ceftazidine pentahydate applied hexamethyldisilazane as protection reagent and new technique of eliminating impurity.Results and conclusion The structure of the target compound was confirmed by IR,^1H-NMR,^13C-NMR.The process is stable,safe and convenient and it is suitable for manufacture.
出处
《中国药物化学杂志》
CAS
CSCD
2010年第3期198-200,共3页
Chinese Journal of Medicinal Chemistry
关键词
头孢菌素
头孢他啶
合成
工艺改进
cephalosporins
ceftazidine
synthesis
process improvement
