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The regioselective coupling of 2-arylquinazolinone C–H with aldehydes and benzyl alcohols under oxidative conditions

The direct and regioselective palladium-catalyzed dehydrogenative coupling of aldehydes and benzyl alcohols with 2-aryl-quinazolinone C–H endowed with a quinazolinone nucleus, which is one of the most fascinating and vital core units, as an inherent directing group under oxidative conditions was developed. This atom/step economic aroylation offers an attractive handle and a very green approach for highly convergent and diversity-oriented synthetic modifications and the construction of vital molecules of therapeutic interest.