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4-[N-甲基-N-(2,3-环氮丙基)]氨基苯甲酸乙酯和N-{4-[N-甲基-N-(2,3-环氮丙基)]氨基}苯甲酰基-L-谷氨酸二乙酯的合成

邓喜玲, 张志丽, 王孝伟, 刘俊义*

  

  1. 1. 北京大学医学部 天然药物及仿生药物国家重点实验室, 北京 100191
    2. 北京大学医学部 药学院 化学生物学系, 北京 100191
    3. 石河子大学 药学院 药学系, 新疆 石河子 832002

  • 收稿日期:2009-10-24 修回日期:2010-02-20 出版日期:2010-03-15 发布日期:2010-03-15
  • 通讯作者: 刘俊义*

Efficient synthesis of ethyl 4-[N-methyl-N-(2,3-aziridinyl)amino]benzoate and diethyl N-{4-[N-methyl-N-(2,3-aziridinyl)amino]benzoyl}-L-glutamate

Xi-Ling Deng, Zhi-Li Zhang, Xiao-Wei Wang, Jun-Yi Liu*

  

  1. 1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China
    2. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    3. Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences, Shihezi University, Xinjiang 832002, China
  • Received:2009-10-24 Revised:2010-02-20 Online:2010-03-15 Published:2010-03-15
  • Contact: Jun-Yi Liu*

摘要: 氮丙啶及其氮取代衍生物能与生物大分子发生亲核开环, 使生物大分子烷基化而失去生物功能。为此我们设计了4-[N-甲基-N-(2,3-环氮丙基)]氨基苯甲酸乙酯和N-{4-[N-甲基-N-(2,3-环氮丙基)]氨基}苯甲酰基-L-谷氨酸二乙酯, 作为进一步合成新型抗肿瘤化合物的重要中间体, 并通过四步反应以较高的收率成功地完成了其合成工作。

关键词: 氮丙啶衍生物, 新型抗肿瘤化合物, 中间体, 合成

Abstract:

Aziridine and its N-substituted derivatives could undergo nucleophilic ring opening reaction with biological molecules, leading to their alkylation and the loss of their biological activities. For this purpose, ethyl 4-[N-methyl-N-(2,3-aziridinyl)amino]benzoate and diethyl N-{4-[N-methyl-N-(2,3-aziridinyl)amino]benzoyl}-L-glutamate, as the key intermediates in the synthesis of new anticancer agents, were designed and synthesized via four steps of reactions in good yields.

Key words: Aziridine derivatives, Intermediates, Anticancer agents, Synthesis

中图分类号: 

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20672008) and 985 Program of Ministry of Education of China.
*Corresponding author. Tel.: 86-10-82801706