【摘要】 建立了一种合成四氢嘧啶衍生物的方法.仲胺与丙炔酸甲酯发生Michael加成反应,生成β-胺基丙烯酸酯;向β-胺基丙烯酸甲酯及亚胺的混合物中加入有机酸,常温下数分钟内发生环合反应得到四氢嘧啶衍生物,仲胺以铵盐形式离去.该反应对甲醛亚胺具有良好的适应性.更多还原

【Abstract】 A facile method for the synthesis of tetrahydropyrimidines is described. Diethylamine was treated with methyl propiolate to provide Michael adduct(β-amino acrylate). In the presence of organic acid, the cyclization of imines with β-aminoacrylateoccurred at room temperature and completed within several minutes to give tetrahydropyrimidines with liberation of ammonium salt. Formaldimines show good toleration to the reaction.更多还原