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](http://hg.y866.cn/compound/lib/scimg/usr/1/C8QO01039K.jpg)
