Iridium‐Catalyzed Site‐ and Enantioselective C(sp2)‐H Borylation of Benzhydryl Ethers: Enantioselectivity Amplification by Kinetic Resolution Relay

Abstract

Comprehensive SummaryWe herein report a simple ether‐directed iridium‐catalyzed site‐ and enantioselective C(sp2)‐H borylation of benzhydryl ethers for the first time. Various chiral benzhydryl ethers were obtained with high enantioselectivities in the presence of a tailor‐made chiral bidentate boryl ligand. We found that the kinetic resolution relay significantly amplified the enantioselectivity. The synthetic utility of the current method was demonstrated by gram‐scale C—H borylation and C—B bond transformations.