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 ...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.展开更多
基金National Natural Science Foundation of China (Grant No.20672008)985 Program of Ministry of Education of China.
文摘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.