A one-pot method for joining three separate components leading to an assortment of 4-arylquinazolines (27 examples) in good to excellent yields is described. The method consists of a palladium(II)-catalyzed cascade reaction involving C(sp)–C(sp2) coupling followed by intramolecular C–N bond formation. The reaction was readily scaled up to gram quantity and successfully applied to the synthesis of a translocator protein (TSPO) ligand.
Key words
4-arylquinazolines - palladium(II) catalysis - one-pot assembly - tandem cyclization reaction - ligands