Asymmetric Organocatalytic Aza-Friedel-Crafts Reaction of Naphthols with N-Sulfonyl Imines

The first organocatalytic asymmetric aza-Friedel-Crafts reaction of naphthols with N-sulfonyl imines has been developed. The cupreine-derived bifunctional organocatalyst BzCPN efficiently catalyzes the formation of aza-Friedel-Crafts prod-ucts in good to excellent yields (up to 99%) with high enantioselectivities (up to 99.5: 0.5 er) under mild reaction conditions, with a low catalyst loading (2-5 mol-%), and in an aerobic environment.