Integrating C-H activation/2-fold annulation: a modular access to heteroaryl-tethered oxazoloisoquinolinones

A cascade C-H activation/2-fold annulation of 2-aryloxazolines with pyridotriazoles has been achieved employing Rh-catalysis to afford heteroaryl-tethered oxazoloisoquinolinones. The synergistic annulations, functional group tolerance, and late-stage skeletal editing of the bioactive scaffolds are the salient practical features.