Dual Inert C–H Bond Site-Selective Activations Enabled by Pd/Norbornene-Mediated Cascade Cyclization toward Medium-Sized Polyheterocyclic Methylene Sulfoximines

A Pd/norbornene-mediated three-component modular one-step reaction facilitated by dual C-H bond activation and cascade cyclization is reported. This procedure uses norbornene as a catalyst in the Catellani-type reaction and as an alkylating building block to accomplish the dual unactivated C-H bond functionalization protocol, which results in the production of polyheterocyclic eight-membered sulfoximines with an indene-fused moiety. This mild, scalable protocol's wide substrate range makes it ideal for site-selective dual C-H functionalization at the highly chemoselective aryl sites.