本文根据二氢叶酸还原酶(DHFR)抑制剂与酶的结合方式,以及可能产生双重抑制作用和长效作用的原理,设计合成了以下三类化合物:Ⅰ、双 -(2,4-二氨基喹唑啉-6-取代氨甲基)芳烃;Ⅱ、1,4-双〔ω-2,4-二氨基喹唑琳-6-取代氨基烷基〕哌嗪;Ⅲ、双-〔4-(2,4-二氨基喹唑啉-6)哌嗪-1〕烷烃或芳烷烃。所合成的29个目的物中,有28个未知化合物,经元素分析、光谱分析确证其结构。化合物I_(1～5)的合成,采用前此未见报道的2,4,6-三氨基喹唑琳与α,α′-二卤代甲基 In this paper, the following three compounds were designed and synthesized according to the binding mode of dihydrofolate reductase (DHFR) inhibitors and enzymes and their possible double inhibition and long-term effects: Ⅰ, bis- (2,4-diamino Quinazoline-6-substituted aminomethyl) arene; II, 1,4-bis [omega-2,4-diaminoquinazolin-6-substituted aminoalkyl] piperazine; (2,4-diaminoquinazolin-6) piperazine-1] alkane or aralkane. Among 29 synthesized objects, 28 unknown compounds were confirmed by elemental analysis and spectral analysis. The synthesis of compounds I_ (1 ~ 5) using the previously reported 2,4,6-triaminoquinazoline and α, α’-dihalomethyl