Quinazoline Synthesis via Rh(III)-Catalyzed Intermolecular C-H Functionalization of Benzimidates with Dioxazolones.

An efficient double C-N bond formation sequence to prepare highly substituted quinazolines utilizing benzimidates and dioxazolones under the catalytic redox-neutral [Cp*RhCl2]2/AgBF4 system, where dioxazolones could work as an internal oxidant to maintain the catalytic cycle, is reported. N-Unsubstituted imine not only acts as a directing group but also functions as a nucleophile in postcoupling cyclization, and dioxazolone acts as a coupling partner for access to heterocycle.