A 纬-carbon activation method that operates through N-heterocyclic carbene/Br酶nsted acid cooperative catalysis for highly enantioselective synthesis of 未-lactams is reported. The protocol allows the challenging remote 纬-carbon control of regioselectivity and enantioselectivity through introduction of an appropriate 纬-leaving group in the enals. The reaction offers good yields and excellent enantioselectivities, and the resulting cyclic products can be easily converted into high-value drug-like derivatives.