Expedient Access to 2-Benzazepines by Palladium-Catalyzed C-H activation: Identification of a Unique HSP90 Inhibitor Scaffold

Bioactive 2-benzazepines were accessed in an atom- and step-economical manner by a versatile palladium-catalyzed C-H activation strategy. The C-H arylation featured low catalyst loading and a mild base being reflected by ample scope and high functional group tolerance. Thereby, the benzotriazolodiazepinones were identified as novel HSP90 inhibitor lead compounds, with considerable potential for anti-cancer applications.