Transition Metal-Catalyzed C−H Activation/Annulation Approaches to Isoindolo[2,1-b]isoquinolin-5(7H)-ones

The isoindolo[2,1-b]isoquinolin-5(7H)-one scaffold is widely present in lots of bioactive natural products. Diverse types of strategies have been developed to construct this scaffold. Recently, transition metal-catalyzed C−H activation/annulation is emerging as a powerful and straightforward method to construct diverse polyheterocycles with high atom- and step-economy. It also has been employed for the synthesis of the isoindolo[2,1-b]isoquinolin-5(7H)-one scaffold. This review provides an introduction to recent advances for the preparation of isoindolo[2,1-b]isoquinolin-5(7H)-ones by using transition metal-catalyzed C−H activation/annulation. It will help researchers to find hidden opportunities and accelerate the discovery of novel transformations based on C−H activation/annulation. © 2023 The Chemical Society of Japan & Wiley-VCH GmbH.