Modular Approach to Substituted Pyridoazepinones

Pyridoazepinones are potentially interesting structures, yet they still underexploited in the medicinal chemistry field and hard to obtain synthetically. We present a general flexible synthetic route substituted pyridoazepinones, enabled by xanthate addition–transfer process, which furnishes target molecules from readily available starting materials generally good yields. The method shows functional group tolerance allows preparation of pyridoazepinone scaffolds on gram scale.