Synthesis of benzo[4,5]imidazo[1,2-a]quinoxalines by I2-mediated sp3 C–H amination

Benzo[4,5]imidazo[1,2-a]quinoxaline derivatives were synthesized from readily accessible 2-(benzoimidazol-1-yl)aniline substrates by an I2-mediated direct sp3 C–H amination reaction. This synthetic strategy does not use transition-metals, is operationally simple and scalable, and gives high yields.