Chiral Catalysts for Pd0‐Catalyzed Enantioselective C−H Activation

Abstract In the past few decades, processes that involve transition‐metal catalysis have represented a major part of the synthetic chemist′s toolbox. Recently, the interest has shifted from the well‐established cross‐coupling reactions to C−H bond functionalization, thus making it a current frontier of transition‐metal‐catalyzed reactions. Constant progress in this field has led to the discovery of enantioselective methods to generate and control various types of stereogenic elements, thereby demonstrating its high value to generate scalemic chiral molecules. The present review is dedicated to enantioselective Pd 0 ‐catalyzed C−H activation, which may be considered as an evolution of Pd 0 ‐catalyzed cross‐couplings, with a focus on the different chiral ligands and catalysts that enable these transformations.