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

AbstractThe 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.