Ligand‐Enabled Pd‐Catalyzed Enantioselective C−H Amination for the Synthesis of Axially Chiral Biaryl Diamines

Pd‐catalyzed enantioselective C−H amination of biaryl amines with morpholino benzoate has been achieved using a novel class of axially chiral diamine ligands featuring a binaphthyl skeleton. The reaction proceeds under very mild conditions and exhibits good functional group tolerance, delivering a range of axially chiral biaryl diamine derivatives bearing a morpholine unit in moderate to good yields (up to 79%) and with good enantioselectivity (up to 90.5:9.5 enantiomeric ratio (er)).