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Copper-catalyzed radical methylation/C-H amination/oxidation cascade for the synthesis of quinazolinones.

A copper-catalyzed radical methylation/sp(3) C-H amination/oxidation reaction for the facile synthesis of quinazolinone was developed. In this cascade reaction, dicumyl peroxide acts not only as a useful oxidant but also as an efficient methyl source. Notably, a methyl radical, generated from peroxide, was confirmed by electron paramagnetic resonance for the first time.