Gold-Catalyzed C(sp2)-H Bond Functionalization

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[[sup]]2[[/sup]])-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[[sup]]2[[/sup]])-H bond functionalization and exhibits the different chemo- and site-selectivities under various reaction conditions.