摘要
以7-ACA为起始原料,经六甲基二硅胺烷保护羧基和氨基、三甲基碘硅烷进行取代后与N-甲基吡咯烷反应以及脱保护制得(6R,7R)-7-氨基-3-[(1-甲基-1-吡咯烷)甲基]头孢-3-烯-4-羧酸盐酸盐,再以丙酮为溶剂与苯并噻唑硫醇活性酯(MAEM)缩合制得盐酸头孢吡肟,总收率59.4%。
Cefepime hydrochloride was synthesized from 7-ACA by protection with ((CH3)3Si)2NH, substitutionwith (CH3)3SiI , reaction with N-methylpyrrolidine and then deprotection to give (6R,7R)-7-amino-3-[(1-methylpyrrolidinyl)methyl]cepha-3-ene-4-carboxylic acid hydrochloride, which subjected to condensation with MAEM in acetone with anoverall yield of 59.4%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2004年第9期515-516,共2页
Chinese Journal of Pharmaceuticals
