Direct Access to α,β-Unsaturated Ketones via Rh/MgCl2-Mediated Acylation of Vinylsilanes

We report herein the facile and practical construction of alpha,beta-unsaturated ketones via rhodium-catalyzed direct acylation of vinylsilanes with readily available and abundant carboxylic acids. This protocol features access to a diverse array of synthetically useful functionalities with moderate to excellent yields. More importantly, the late-stage functionalization of pharmaceuticals was also realized with synthetically useful yield.

Automated summary

A new method using rhodium-catalyzed direct acylation has been developed for the construction of alpha,beta-unsaturated ketones, providing access to a variety of synthetically useful functionalities with high yields. Importantly, this method is also applicable for late-stage functionalization of pharmaceuticals with high yields.