Direct Catalytic Enantioselective Hydrophosphonylation of N-Unsubstituted Ketimines

We report a direct catalytic enantioselective hydrophosphonylation of N-unsubstituted ketimines that affords N-unprotected α-tetrasubstituted α-aminophosphonates without protection/deprotection steps. The reaction is suitable for N-unsubstituted isatin-derived ketimines and N-unsubstituted trifluoromethyl ketimines, affording products in high yields with excellent enantioselectivity. Applications of the reaction and a proposed transition state model are also described.