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  

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(英文)

作　　者：邓喜玲[1,2] 张志丽[1] 王孝伟[1] 刘俊义[3,1] 

机构地区：[1]北京大学医学部药学院化学生物学系,北京100191 [2]石河子大学药学院药学系,新疆石河子832002 [3]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

出　　处：《Journal of Chinese Pharmaceutical Sciences》2010年第2期141-145,共5页中国药学（英文版）

基　　金：National Natural Science Foundation of China (Grant No.20672008);985 Program of Ministry of Education of China.

摘　　要：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.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：Aziridine derivatives Intermediates Anticancer agents Synthesis 

分 类 号：TQ245.24[化学工程—有机化工]