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Abstract Amide is one of the most widespread functional groups in organic and bioorganic chemistry, and it would be valuable to achieve stereoselective C(sp 3 )−H functionalization in amide molecules. Palladium(II) catalysis has been prevalently used in the C−H activation chemistry in the past decades, however, due to the weakly‐coordinating feature of simple amides, it is challenging to achieve their direct C(sp 3 )−H functionalization with enantiocontrol by Pd II catalysis. Our group has developed sulfoxide‐2‐hydroxypridine (SOHP) ligands, which exhibited remarkable activity in Pd‐catalyzed C(sp 2 )−H activation. In this work, we demonstrate that chiral SOHP ligands served as an ideal solution to enantioselective C(sp 3 )−H activation in simple amides. Herein, we report an efficient asymmetric Pd II /SOHP‐catalyzed β‐C(sp 3 )−H arylation of aliphatic tertiary amides, in which the SOHP ligand plays a key role in the stereoselective C−H deprotonation‐metalation step.
Yuan et al. (Sun,) studied this question.