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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.
A method for the synthesis of tetrahydropyrimidine derivatives was established.The Michael addition reaction of the secondary amine and methyl propiolate to produce β-aminoacrylate; to a mixture of β-aminoacrylate and imine The organic acid, ring-closure reaction within a few minutes at room temperature to give tetrahydropyrimidine derivatives, the secondary amine to leave the ammonium salt form. The reaction of formaldehyde imine has good adaptability.