中文摘要：

以2-溴丙酸甲酯、α,α-二氯甲基甲醚和胍唑为原料，经缩合以及环化反应制得2-氦基-6-甲基-5-氧代-4，5-二氢-1，2，4-三氮唑并[1，5-a]嘧啶．为了提高其在有机溶剂中的溶解性，该化合物再同1-溴丁烷发生亲核取代反应得到了2-氨基-6-甲基-5-氧代-4-正丁基-4，5-二氢-1，2，4-三氮唑并[1，5-a]嘧啶，然后与芳基醛和叔丁基异氰发生Ugi多组分反应，合成了一系列具有潜在催吐活性的2-取代氨基-6-甲基-5-氧代-4-正丁基-4，5-二氢-1，2，4-二氮唑并[1，5-a]嘧啶类衍生物，产品结构经质谱、核磁其振谱及元素分析确认．

英文摘要：

2-Amino-6-methyl-5-oxo-4,5-dihydro-1,2,4-triazolo[1,5-a]pyrimidine was synthesized from 2-bromopropionic acid methyl ester, α,α-dichloromethyl methyl ether and guanazole via condensation and cyclization reactions. An attempt to improve its solubility in organic solvents was achieved by the nucleophilic substitution with 1-bromobutane to give 2-amino-4-n-butyl-6-methyl-5-oxo-4,5-dihydro-1,2,4-triazolo [1,5-a]pyrimidine in a good yield. Finally, a series of 2-（substituted amino）-4-n-butyl-6-methyl-5-oxo-4,5- dihydro-1,2,4-triazolo[1,5-a]pyrimidines having potential emetic activity were obtained by Ugi multi-component reactions. The structures of these compounds were confirmed by MS, ^1H NMR and ^13C NMR spectra and elemental analysis.