The lipase-catalyzed asymmetric resolution of 2-azabicyclo [2.2. 1] hept-5-en-3-ones is reported; non-racemic chiral 2-azabicyclo [2.2. 1] hept-5-en-3-ones were obtained conveniently by lipase-catalyzed enantioselective transesterification or hydrolysis of N- hydroxymethyl-2-azabicyclo [2.2. 1] hept-5-en-3-one or N-acyloxymethyl-2-azabicyclo [2.2. 1] hept-5-en-3-one.