Modular Approach to Substituted Pyridoazepinones

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