中文摘要：

报道了N-{4-{N-甲基-N-[2-羟基-3-（2，4-二氧代-1，2，3，4-四氢嘧啶-5-基）氨基]丙基}氨基-3-溴}苯甲酰基-L-谷氨酸二乙酯及其衍生物的简便合成方法．分别以4-氨基苯甲酸乙酯和4-氨基苯甲酰基也．谷氨酸二乙酯为起始物，经甲基化、烯丙基化、溴羟基化、环氧化、开环、脱保护等反应首次合成了6个新型5-取代氨基嘧啶类化合物，并通过^1H NMR，^13C NMR和MS对其化学结构进行了表征．初步生物活性结果表明，苯环侧链的L-谷氨酸酯部分是此类化合物抑制人重组二氢叶酸还原酶的必需结构．

英文摘要：

A new practical approach to prepare diethyl N-{4-[N-methyl-N-（3-（2,4-dioxo-l,2,3,4-tetrahydropyrimidin-5-yl）amino-2-hydroxypropyl）amino]benzoyl}-L-glutamate and its derivatives has been realized from ethyl 4-aminobenzoate （4a） and diethyl N-（4-aminobenzoyl）-L-glutamate （4b）. Six novel 5-（substituted）amino pyrimidines 9-11 were synthesized via methylation, allylation, bromohydroxylation, epoxidation, ring-opening, deprotection reaction and so on, and were characterized by ^1H NMR, ^13C NMR and MS techniques. The inhibitory activities against human dihydrofolate reductase of the compounds have been determined. The results showed that the bioactivities of the compounds were related with L-glutamate side chain.