Asymmetric C–H hydroarylation and annulation cascade for the skeletal diversification of dihydrofuran-fused-phthalimides

Abstract

We report a Ru(II)-catalyzed enantioselective C(aryl)–H hydroarylation–annulation cascade with isocyanates for the synthesis of structurally diverse dihydrofuran-fused phthalimides. A chiral sulfoximine directing group ensures high enantioselectivity (up to 97 : 3 er). The method exhibits broad substrate scope and is scalable to the gram scale, offering access to construct complex enantioenriched heterocycles.