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

Sylvain Laclef (1) , Marine Harari (1) , Julien Godeau (1) , Isabelle Schmitz-Afonso (1) , Laurent Bischoff (1) , Vincent Levacher (1) , Christophe Hoarau (1) , Corinne Fruit (1) , Thierry Besson (1)

1 COBRA - Chimie Organique et Bioorganique : Réactivité et Analyse

A microwave-assisted method for the palladiumcatalyzeddirect arylation of quinazolin-4-one has beendeveloped under copper-assistance. This method is applicableto a wide range of aryl iodides and substituted (2H)-quinazolin-4-ones. This protocol provides a simple and efficient way tosynthesize biologically relevant 2-arylquinazolin-4-one backbones.

Domaines: Chimie organique; Catalyse

Sylvain Laclef, Marine Harari, Julien Godeau, Isabelle Schmitz-Afonso, Laurent Bischoff, et al.. Ligand-Free Pd-Catalyzed and Copper-Assisted C−H Arylation ofQuinazolin-4-ones with Aryl Iodides under Microwave Heating. Organic Letters, 2015, organic letters, 17 (7), pp.1700-1713. ⟨10.1021/acs.orglett.5b00467⟩. ⟨hal-01141150⟩