乙烯酯与脂肪胺的酰胺化反应

The Amidation of Vinyl Esters with Aliphatic Amines

酰胺化合物广泛存在天产产物、药物和生物体中,在有机合成中有着广泛的应用,由简单和易制备的原料摸索一种环境友好、高效合成酰胺的方法是很有意义的。本文以醋酸乙烯酯和苯甲酸乙烯酯为酰化试剂,在60℃、甲苯作为溶剂条件下可以顺利与伯胺、仲胺及含有杂环的胺反应,高效构筑酰胺键,以63%-100%的产率合成12种酰胺类化合物;该反应可以放大50倍,达到6.7 g级规模而且可以保持较高的产率。该反应不需任何催化剂且操作简单,条件温和,这为酰胺化合物的制备提供了一个绿色经济及简单的方法,并且具有一定的工业应用前景。

Amides are widely present in the natural products,drugs and organism and has been widely use in organic synthesis. The development of environmentally benign and efficient method for the synthesis of amides from readily available and simple substrate is still highly significant.In this paper,vinyl acetate and vinyl benzoate as acylating agents,reacted smoothly with primary amines,secondary amines and heterocyclic amines in toluene to give 12 amides in 63%-100% yields under 60 ~C to construct the amide bonds efficiently.On the other hand,this reaction can be scaled up 50 times easily and achieve 6.7 gram while maintaining a high yield. It has advantage of simple operation,mild conditions,without catalyst,which provides a green economy method for the preparation of amides compounds and has prospects in the industrial application.