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盐酸头孢吡肟的合成
引用本文:王红波,杨银萍,赵荐飞. 盐酸头孢吡肟的合成[J]. 齐鲁药事, 2012, 31(2): 70-71
作者姓名:王红波  杨银萍  赵荐飞
作者单位:1. 鲁南制药集团股份有限公司,山东,临沂,276006
2. 临沂大学化学实验中心,山东,临沂,276003
摘    要:以7-ACA为起始原料,在环己烷中用六甲基二硅氨烷(HMDS)和三甲基碘硅烷(TMSI)将7-ACA中的氨基和羧基硅烷化,然后与N-甲基吡咯(NMP)和TMSI的反应产物混合,生成(6R,7R)-7-氨基-3-[(1-甲基-1-吡咯烷鎓盐)甲基]头孢-3-烯-4-羧酸氢碘酸盐(中间体Ⅱ),再与活性酯反应得到盐酸头孢吡肟。

关 键 词:盐酸头孢吡肟  抗生素  头孢菌素  合成

Synthesis of cefepime hydrochloride
WANG Hong-Bo,YANG Yin-Ping,ZHAO Jian-Fei. Synthesis of cefepime hydrochloride[J]. qilu pharmaceutical affairs, 2012, 31(2): 70-71
Authors:WANG Hong-Bo  YANG Yin-Ping  ZHAO Jian-Fei
Affiliation:WANG Hong-Bo, YANG Yin-Ping, ZHAOJtan-Fei ( 1. Lunan Pharmaceutical Co. , Ltd. , Linyi 276006, China ;2. Chemical Experiment Center, Linyi University, Linyi 276003, China )
Abstract:Cefepime hydrochloride was synthesized with 7 -ACA as the starting material. At first ,7 -ACA was protected by hexamethyldisilazane ( HMDS ) and iodotrimethylsilane ( TMSI ) in cyclohexane, and was reacted with the product of N - methylpyr- rolidine ( NMP ) and iodotrimethylsilane to synthesize ( 6 R,7 R ) - 7 - amino - 3 - [ ( 1 - methyl - 1 - pyrrolidinio ) methyl ] ceph - 3 -em - 4 - carboxylate monohydriodide (Ⅱ ) , and then reacted with an active ester to obtain cefepime hydrochloride.
Keywords:Cefepime hydrochloride  Antibacterial  Cephalosporin  Synthesis
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