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

J Org Chem. 2015 May 1;80(9):4736-42. doi: 10.1021/acs.joc.5b00191. Epub 2015 Apr 20.

Abstract

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.