Catalyst-Free Transamidation of Aromatic Amines with Formamide Derivatives and Tertiary Amides with Aliphatic Amines
作者:Jiawen Yin、Jingyu Zhang、Changqun Cai、Guo-Jun Deng、Hang Gong
DOI:10.1021/acs.orglett.8b03542
日期:2019.1.18
A simple catalyst- and promoter-free protocol has been developed for the transamidation of weakly nucleophilic aromatic amines with formamide derivatives and low-reactivity tertiary amides with aliphatic amines. This strategy is advantageous because no catalyst or promoters are needed, no additives are required, separation and purification is easy, and the reaction is scalable. Significantly, this
已经开发了一种简单的无催化剂和无助催化剂的方案,用于弱亲核芳香胺与甲酰胺衍生物的酰胺交换,以及低反应性叔酰胺与脂族胺的酰胺交换。该策略是有利的,因为不需要催化剂或助催化剂,不需要添加剂,分离和纯化容易,并且反应是可扩展的。重要的是,该策略被进一步应用于以克为单位合成几种药物分子,并获得了优异的收率。