以乙酰乙酸乙酯为原料进行环合反应,生成2-氨基-4-羟基-6-甲基嘧啶,然后在三氯氧磷的作用下进行羟基氯代,再与氨基化合物反应得到一系列的2,4,6-三取代嘧啶类衍生物(4a~4f),并采用IR、ESI-MS和1 H NMR对其结构进行了表征。考察了氯代反应中氯代试剂、温度、时间等因素对合成收率的影响。结果表明,氯代反应的较佳条件是:三氯氧磷为氯代试剂,反应温度40℃,反应时间12 h,氯代产物收率达84.8%。%With ethyI acetyIacetate as raw materiaI,synthetic strategy was compIeted by cycIization reac-tion,chIorination,and amination,six noveI 2,4,6-trisubstituted pyrimidine derivative(4a~4f)were syn-thesized,the structures were characterized by IR,ESI-MS and 1 H NMR. The affecting of chIorinated rea-gent,temperature and time etc. on synthesis yieId were investigated. The resuIts show that the better reac-tion conditions of the chIorinated reaction are as foIIows:POCI3 is chIorinated reagents,the reaction tem-perature is 40 ℃,the action time is 12 h,and the chIorinated reaction yieId can reach 84. 8%.
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