Copper‐Catalyzed sp ² CH Bond Functionalization

Abstract

The use of sp 2 CH bonds as key functional groups has been realized by transition metal‐mediated CH bond activation and functionalization. In this regard, copper‐catalyzed CH activation has emerged as an environmentally benign and economically attractive approach in modern synthetic organic chemistry. Copper salts serve as versatile catalysts for oxidative coupling reactions and are often proposed to serve as a one‐electron oxidant to promote the single‐electron transfer process. This article discusses the recent advances in the copper‐catalyzed sp 2 CH functionalization achieving CC, CN, CO, CS, and CX bond formation via direct CH activation as well as directing group‐assisted activation strategy. An understanding of the mechanism of these reactions involving organocopper intermediates is crucial to promote the discovery of efficient and highly selective catalytic systems.