Rh(III)-catalyzed twofold unsymmetrical C H alkenylation-annulation/amidation reaction enabled delivery of diverse furoquinazolinones

Multiple functionalized arenes are irreplaceable part of numerous bioactive natural products and pharmaceuticals. Transition-metal-catalyzed direct unsymmetrical twofold or multiple C H bonds functionalization was highly desirable but less explored. Herein, we have developed a Rh(III)-catalyzed unsymmetrical C H alkenylation-annulation/amidation reaction with a O -bearing olefin-tethered arenes, enabling delivery of diverse furoquinazolinones in one step with broad substrate scope and good functional group tolerance.