Abstract

Here, we have developed an expeditious and efficient protocol for the synthesis of isoxazole-5(4H)-ones derivatives using guanidine hydrochloride as a catalyst using water as a solvent. The one-pot multicomponent reaction of aldehydes, ethyl acetoacetate, and hydroxylamine hydrochloride at room temperature to give a 3-methyl-4-(hetero)arylmethylene isoxazole-5(4H)-ones derivatives in an excellent yield. The key advantages of the reported method are shorter reaction time, energy-efficient, easy work-up procedure, wide substrate scope tolerance, economical, etc. further the catalyst was recycled up to 5 times along with high product yield without significant loss of its catalytic activity.

摘要

在这里，我们开发了一种使用盐酸胍作为催化剂，以水为溶剂，合成异恶唑-5(4H)-ones 衍生物的快速有效的方案。醛、乙酰乙酸乙酯和盐酸羟胺在室温下进行一锅多组分反应，以优异的收率得到 3-甲基-4-(杂)芳基亚甲基异恶唑-5(4H)-酮衍生物。所报道的方法的主要优点是反应时间短、能源效率高、后处理程序容易、底物范围宽、经济等。此外，催化剂可循环使用多达 5 次，产品收率高，且不会显着损失催化剂。催化活性。