Direct CH Difluoroalkylation and Perfluoroalkylation of Heteroarenes

Abstract This article summarizes the main recent achievements reported in transition metal‐catalyzed and metal‐free CH difluoromethylation and perfluoroalkylation using various fluoroalkyl‐coupling partners over the past decade, for constructing high‐valuable fluoro‐containing heteroarenes. This resume is mainly categorized based on different catalytic systems for each fluoroalkylation reaction. Difluoroalkylation that involves a metal‐catalyzed or a visible‐light‐induced reaction will be addressed first. Following this, the direct perfluoroalkylation of CH bonds under various reaction conditions will be covered. The overall aim is to paint a picture of the state of the art in difluoro‐ and perfluoroalkylation chemistry for medicinal chemists and point out how the recent innovative strategies have been able to positively affect the synthesis of new bioactive compounds.