摘要

Reported herein is the pyrazole‐directed iridium‐catalyzed enantioselective borylation of unbiased methylene C?H bonds at the position β to a nitrogen center. The combination of a chiral bidentate boryl ligand, iridium precursor, and pyrazole directing group was responsible for the high regio‐ and enantioselectivity observed. The method tolerated a vast array of functional groups to afford the corresponding C(sp3)?H functionalization products with good to excellent enantioselectivity.