锌介导的炔酰胺串联氧化/卤化反应合成α-卤代酰胺

Synthesis of α-Halo Amides via Zinc-Mediated Tandem Oxidation/Halogenation of Ynamides

α-卤代酰胺是一类十分重要的羰基化合物,广泛存在于众多天然产物和生物活性分子之中.本工作实现了通过卤化锌同时作为催化剂和卤素源的炔酰胺串联氧化/卤化反应,从而避免使用其他的外加卤化试剂.该反应可以中等到良好的产率得到一系列合成上非常有用的α-卤代酰胺化合物.

α-Haloamides are a very important class of carbonyl compounds,and widely exist in a range of natural products and bioactive molecules.Herein,the realization of the tandem oxidation/halogenation of ynamides by employing the zinc halide as both the catalyst and the halogen source is described,thus avoiding the use of other external halogenating reagents.This method allows the practical synthesis of a variety of valuableα-haloamides in moderate to good yields.