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A highly regioselective C–C bond cleavage/amination of isatins has been developed for the synthesis of benzimidazo[1,2-c]quinazolin-6-ones by reacting with o-phenylene diamines. This practical transition-metal-free method is operationally simple, enabling the C–C bond cleavage and triple C–N bond formation, wherein molecular oxygen is the sole required oxidant.

Graphical abstract: Direct construction of benzimidazo[l,2-c]quinazolin-6-ones via metal-free oxidative C–C bond cleavage

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