Pd-catalyzed alpha-olefinic C-H activation of simple alpha,beta-unsaturated olefins has been developed. 4-imino-beta-lactam derivatives were readily synthesized via activation of alpha-olefinic C-H bonds with excellent cis stereoselectivity. A wide range of heterocycles at the beta-position are compatible with this reaction. The product of 4-imino-beta-lactam derivatives can be readily converted to 2-aminoquinoline which exists extensively in pharmaceutical drugs and natural products.