An Approach to Vinylidenequinazolines from Isoxazoles and Dioxazolones

An effective strategy for the synthesis of vinylidenequinazolines has been efficaciously developed, which involves Rh­(III)-assisted C–H amidation followed by ring-opening and intramolecular annulation. This protocol shows a straightforward way to construct diverse quinazoline units with a wide functional group compatibility from readily available isoxazoles and dioxazolones.