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A palladium-catalyzed oxidative coupling reaction constitutes an attractive approach for synthesis of 2,3-disubstituted quinazolinones. However, poor functional group tolerance, low selectivity, and side reactions have hindered their practical application. Herein, using methyl anthranilates, isocyanides and arylboronic acids, an atom-economy cascade protocol for the synthesis of 2,3-disubstituted quinazolinones via NHC–palladium-catalyzed oxidative coupling reactions has been developed with a broad substrate scope and good functional group tolerance.

Graphical abstract: Cascade synthesis of 2,3-disubstituted quinazolinones from methyl anthranilates, isocyanides and arylboronic acids via NHC–palladium-catalyzed oxidative coupling reactions

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