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)

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。