C–H bonds are common in organic molecules, and the functionalization of these inactive C–H bonds has become one of the most powerful methods used to assemble complicated bioactive molecules from readily available starting materials. However, a central challenge in these reactions is controlling their stereoselectivity. Recently, significant progress has been made in the development of enantioselective C–H activation enabled by different chiral ligands for the formation of C–C and C–X bonds bearing a chiral center. In this paper, we focus on some archetypal chiral ligands for enantioselective C–H functionalization developed in recent years and analyze the mechanism of these methods, aiming to accelerate related research and to search for more efficient strategies.
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