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Ligand-Free Pd-Catalyzed and Copper-Assisted C-H Arylation of Quinazolin-4-ones with Aryl Iodides under Microwave Heating

Sylvain Laclef, Marine Harari, Julien Godeau, Isabelle Schmitz-Afonso, Laurent Bischoff, Christophe Hoarau, Vincent Levacher, Corinne Fruit* and Thierry Besson*

*Normandie Univ, COBRA, UMR 6014 et FR 3038; Univ Rouen; INSA Rouen; CNRS, IRCOF, 1 rue Tesnière, 76821 Mont Saint Aignan Cedex, France, Email:,

S. Laclef, M. Harari, J. Godeau, I. Schmitz-Afonso, L. Bischoff, C. Hoarau, V. Levacher, C. Fruit, T. Besson, Org. Lett., 2015, 17, 1700-1703.

DOI: 10.1021/acs.orglett.5b00467 (free Supporting Information)

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A microwave-assisted method for the palladium-catalyzed direct arylation of quinazolin-4-one has been developed under copper-assistance. This method is applicable to a wide range of aryl iodides and substituted (2H)-quinazolin-4-ones. This protocol provides a simple and efficient way to synthesize biologically relevant 2-arylquinazolin-4-one backbones.

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Key Words

quinazolinones, microwave synthesis

ID: J54-Y2015