Gold‐Catalyzed C(sp 2 )H Bond Functionalization

Abstract The direct conversion of CH bond into CX bond has been emergent as an efficient approach for the construction of complex molecules. In this area, gold‐catalyzed C(sp 2 )H bond functionalization has attracted great interest over the past two decades as a synthetic toolbox for the construction of complex molecules and late‐stage modification of bioactive compounds. This article summarizes the evolution of gold‐catalyzed C(sp 2 )H bond functionalization and exhibits the different chemo‐ and site‐selectivities under various reaction conditions.