Rh(III)-Catalyzed Redox-Neutral C–H Activation/Annulation of Oxadiazolones with Sulfoxonium Ylides to access oxadiazoloisoquinolinone

Abstract

Here, we developed a synthetic route for oxadiazolone-fused isoquinoline derivatives through Rh(III)-catalyzed [4+2] redox-neutral annulations of aryl oxadiazolones with sulfoxonium ylides, followed by a second C–H activation to produce acymethylation products. The method provides broad substrate scope, functional group tolerance, and gram-scale synthesis. The resulting compounds exhibited antidiabetic and anti-inflammatory activities, highlighting their therapeutic potential.