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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (13): 1589-1591. 上一篇    

研究简报

去乙酰基-7-氨基头孢烷酸二苯甲酯的合成

王阁, 曹小辉, 于亮, 陈立功*   

  1. (天津大学化工学院 天津 300072)
  • 投稿日期:2010-09-30 修回日期:2011-01-13 发布日期:2011-03-17
  • 通讯作者: 陈立功 E-mail:lgchen@tju.edu.cn
  • 基金资助:

    国家自然科学基金项目

Synthesis of Benzhydryl 7-Amino-3-(hydroxymethyl)-8-oxo-5- thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

WANG Ge, CAO Xiao-Hui, YU Liang, CHEN Li-Gong   

  1. (School of Chemical Engineering, Tianjin University, Tianjin 300072)
  • Received:2010-09-30 Revised:2011-01-13 Published:2011-03-17
  • Contact: Ligong Chen E-mail:lgchen@tju.edu.cn

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被引次数

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头孢卡品酯是第四代头孢类抗菌素的重要品种, 人们已经对以去乙酰基-7-氨基头孢烷酸(D-7ACA)为起始原料合成头孢卡品酯的工作进行了大量研究, 其中大部分都涉及到D-7ACA上羧基的保护, 因此, 对D-7ACA的羧基保护的研究是非常重要的. 以二苯基重氮甲烷和D-7ACA为起始原料, 采用超声波辅助的方法, 以70%的收率合成了去乙酰基-7-氨基头孢烷酸二苯甲酯.

关键词: D-7ACA, 二苯基重氮甲烷, 羧基保护, 头孢卡品酯, 超声波

Cefcapene Pivoxil is important one of the fourth generational cephalosporin antibiotics. The synthesis of Cefcapene Pivoxil from D-7ACA has been intensively studied. Normally, it is involved to protect the carboxyl group of D-7ACA. Thus, it is very important to study the protection of carboxyl group of D-7ACA. Benzhydryl 7-amino-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylate was obtained from D-7ACA with diphenyldiazo-methane as protection reagent, enhanced by ultrasonic wave, in 70% yield.

Key words: D-7ACA, diphenyldiazomethane, carboxyl protection, cefcapene pivoxil, ultrasonic wave