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羰基二咪唑酰化剂用于头孢菌素的合成

APPLICATION OF N,N’-CARBONYLDIIMIDAZOLE TO THE SYNTHESIS OF CEPHALOSPORINS

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【作者】 陈庆平; 段廷汉; 周慧殊;

【Author】 Chen Qingping, Duan Tinghan and Zhou Huishu (Department of Pharmaceutical Chemistry)

【机构】 中国药科大学制药化学教研室; 中国药科大学制药化学教研室;

【摘要】 <正> 头孢菌素合成常采用混合酸酐法、DCC法、活化酯法等肽类合成方法。羰基二咪唑(简称CDI,I)法也属肽类合成方法。最近有文献报道,将此法用于头孢菌素C3·位乙酰氧基的改造以及氨苄青霉素α-氨基的修饰。但用于头孢菌素C7位缩合未见报道。本文采用

【Abstract】 CDI(N,N’-Carbonyldiimidazole) acylating agent was used in direct condensation for the synthesis of cephalosporins. The application of CDI in the preparation of 7β-(6-Substituded-2-quinolone-3-acetamido)-cephalosporins was studied. The reaction conditions under which the synthesis is accomplished were discussed and the preliminary comparison with other methods was made. The method could be satisfactorily applied to the synthesis of cephalosporins, since the procedure was simple and efficient and proved useful particularly for the carboxylic acids with active hydrogen containing-bulky substituted group. The method could also be widely used for the research of semisynthetic cephalosporins.

【关键词】 羰基二咪唑; 酰化; 头孢菌素;
【Key words】 N, N’-Carbonyldiimidazole; Acylation; Cephalosporins;
  • 【文献出处】 中国药科大学学报 ,Journal of China Pharmaceutical University , 编辑部邮箱 ,1988年03期
  • 【被引频次】1
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