An Efficient Protocol for the Amidation of Carboxylic Acids Promoted by Trimethyl Phosphite and Iodine
作者:Qun-Li Luo、Lina Lv、Yu Li、Jian-Ping Tan、Wenhui Nan、Qun Hui
DOI:10.1002/ejoc.201101030
日期:2011.12
A practical, one-pot protocol is described for the conversion of carboxylic acids into amides through carboxyl activation by the reagent combination of trimethyl phosphite and iodine. This method integrates several advantages: (1) it allows amines to be chemoselectively acylated with excellent results in the presence of sulfur and oxygen nucleophiles; (2) the method shows wide generality in respect
描述了一种实用的一锅法,用于通过亚磷酸三甲酯和碘的试剂组合通过羧基活化将羧酸转化为酰胺。这种方法综合了几个优点:(1)它允许胺在硫和氧亲核试剂的存在下被化学选择性地酰化,并获得优异的结果;(2)该方法在溶剂、碱和底物方面具有广泛的通用性;(3) 使用的试剂广泛可用且比普通偶联试剂便宜得多,并且 (4) 该过程非常方便,允许提取、重结晶和柱色谱作为可选的后处理程序。该方法的化学选择性和通用性、成本低、试剂的广泛可用性以及易用性使其成为一个非常有利的过程。