Ruthenium‐Catalyzed Direct Asymmetric Reductive Amination of Diaryl and Sterically Hindered Ketones with Ammonium Salts and H2

A Ru‐catalyzed direct asymmetric reductive amination of ortho‐OH‐substituted diaryl and sterically hindered ketones with ammonium salts is reported. This method represents a straightforward route toward the synthesis of synthetically useful chiral primary diarylmethylamines and sterically hindered benzylamines (up to 97 % yield, 93–>99 % ee). Elaborations of the chiral amine products into bioactive compounds and a chiral ligand were demonstrated through manipulation of the removable and convertible ‐OH group. OH yeah: A highly enantioselective OH‐assisted direct asymmetric reductive amination of diaryl and sterically hindered ketones with ammonium salts and H2 was developed. This reaction has a broad substrate scope (>30 examples) and offers straightforward access to synthetically useful chiral primary diarylmethylamines and sterically hindered benzylamines with high yield and enantioselectivity.