Clickable coupling of carboxylic acids and amines at room temperature mediated by SO<sub>2</sub>F<sub>2</sub>: a significant breakthrough for the construction of amides and peptide linkages
作者:Shi-Meng Wang、Chuang Zhao、Xu Zhang、Hua-Li Qin
DOI:10.1039/c9ob00699k
日期:——
carboxylic acids with amines was developed for the synthesis of a broad scope of amides in a simple, mild, highly efficient, robust and practical manner (>110 examples, >90% yields in most cases). The direct click reactions of acids and amines on a gram scale are also demonstrated using an extremely easy work-up and purification process of washing with 1 M aqueous HCl to provide the desired amides in
酰胺键和肽键的构建是所有生命过程和有机合成中最基本的转变之一。结构无处不在的酰胺基序的合成对于许多重要分子(如肽,蛋白质,生物碱,药剂,聚合物,配体和农用化学品)的组装至关重要。开发了一种SO2F2介导的羧酸与胺的直接可点击偶合方法,以简单,温和,高效,稳健和实用的方式合成各种酰胺(> 110例,大多数情况下> 90%的收率) )。