Transition Metal‐Catalyzed Desymmetrizations Based on CH Activation Processes

Abstract The relevance of chiral pharmaceuticals and fine chemicals has encouraged the development of synthetic methods that allow the preparation of these products in enantioselective form. Of the different strategies, those relying on the metal‐catalyzed enantioselective activation of CH bonds are especially appealing, owing to their step and atom economy. This is particularly the case in desymmetrization approaches, because of the simplicity of the reactants, and their intrinsic complexity increase characteristics. This article reviews the current state of the art on transition metal‐catalyzed desymmetrizing functionalizations involving enantiodetermining CH activation steps.