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We herein report a direct and efficient protocol for phosphorylation of quinoxalines, which employs aerobic oxygen as the green oxidant under catalyst-free conditions. This methodology represents one of the most environmentally friendly and easily handled protocols, providing a series of phosphorylated quinoxalines in good to excellent yields. Control experiments clearly indicated that the reaction followed a dearomatization–rearomatization strategy.

Graphical abstract: Aerobic oxidative C–H phosphorylation of quinoxalines under catalyst-free conditions

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