Abstract:
A highly efficient protocol has been developed for the synthesis of diversely substituted isoindolo[2,1-b]isoquinolin-7(5H)-ones through sequential Cu(II)-catalyzed Sonogashira coupling, intramolecular hydroamidation followed by palladium-catalyzed ligand-free Heck reaction. Good to excellent yields (41–94%) were observed with excellent substrate scope and functional group tolerance. The developed method represents a practical strategy for the construction of bioactive isoindolo[2,1-b]isoquinolin-7(5H)-ones.