青霉素扩环半合成头孢菌素研究进展

Research Progress of Semi-synthetic Cephalosporin by Ring-expansion of Penicillin G

以青霉素为原料经过化学方法扩环半合成头孢菌素中间体包括7-ADCA、GCLE(GCLH)、3-羟基头孢烯、3-环外亚甲基头孢烷酸和丙二烯羧酸酯类氮杂环丁酮.在此基础上综述了各中间体合成相关头孢菌素品种,以及由青霉素扩环制备头霉素和1-氧头孢菌素的研究进展.同时,针对目前该领域的发展状况提出了适合国情的由青霉素半合成头孢菌素一些思路和建议.

Penicillin G is often utilized as an economical starting material to synthesize cephalosporin,which needs many intermediates,such as 7-ADCA,GCLE,GCLH,3-exomethylenecepham,allene carboxylate＇s azetidinone.Varieties of cephalosporin which are synthesized by various intermediate products were reviewed as well as the progress of preparing cephamycin and 1-oxygen cephalosporin by these intermediates.At the same time,in the light of the current developing situation of this field,some ideas and suggestions for semi-synthetic cephalosporin by penicilliums which are appropriate for China＇s national conditions were proposed.