Rh(III)-Catalyzed three-component cascade annulation to produce the N-oxopropyl chain of isoquinolone derivatives.

Developing powerful methods to introduce versatile functional groups at the N-substituents of isoquinolone scaffolds is still a great challenge. Herein, we report a novel three-component cascade annulation reaction to efficiently construct the N-oxopropyl chain of isoquinolone derivatives via rhodium(iii)-catalyzed C-H activation/cyclization/nucleophilic attack, with oxazoles used both as the directing group and potential functionalized reagents.