Synthesis of Aza‐Bicyclic Maleimide Skeleton by Addition‐Ring Opening Cascade Reaction of Vinylogous Oxindole

An efficient method has been developed to facilitate the addition‐ring opening cascade reaction of vinylogous oxindole, resulting in the synthesis of a variety of aza‐bicyclic maleimide derivatives with high yields and exceptional diastereoselectivities. Furthermore, the product could be effectively and easily transformed into the difluoromethylenecyclohexane skeleton through a dehydrofluorination process. This methodology demonstrates significant potential for the synthesis of aza‐bicyclic maleimide skeleton, which possesses biological or pharmaceutical activity.