Iridium‐Catalyzed Regio‐ and Enantioselective Borylation of Unbiased Methylene C(sp3)‐H Bonds at the Position Beta to a Nitrogen Center

Abstract

Reported here is the first example of pyrazole‐directed iridium‐catalyzed enantioselective borylation of unbiased methylene C‐H bonds at the position beta to a nitrogen center. The combination of a chiral bidentate boryl ligand, iridium precursor, and pyrazole directing group is responsible for achieving high regio‐ and enantioselectivities. The current method can tolerate a vast array of functional groups, affording corresponding C(sp 3 )‐H functionalization products in good to excellent enantioselectivities.