Copper-catalyzed domino sequences: a new route to pyrido-fused quinazolinones from 2′-haloacetophenones and 2-aminopyridines

A new pathway to access pyrido-fused quinazolinones via a Cu(OAc) 2 -catalyzed domino sequential transformation between 2′-haloacetophenones and 2-aminopyridines was demonstrated. The solvent and base exhibited a remarkable effect on the transformation, in which the combination of DMSO and NaOAc emerged as the best system. Cu(OAc) 2 ·H 2 O was more active towards the reaction than numerous other catalysts. This methodology is new and would be complementary to previous protocols for the synthesis of pyrido-fused quinazolinones. A new pathway to access pyrido-fused quinazolinones via a Cu(OAc) 2 -catalyzed domino sequential transformation between 2′-haloacetophenones and 2-aminopyridines was demonstrated.