Modular Approach to Substituted Pyridoazepinones

Valentin S Dorokhov (1) , Samir Z Zard (1)

1 DCSO - Laboratoire de synthèse organique

Pyridoazepinones are a potentially interesting structures, yet 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 additiontransfer process, and furnishing 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.

Domaines: Chimie organique

Valentin S Dorokhov, Samir Z Zard. Modular Approach to Substituted Pyridoazepinones. Organic Letters, 2021, 23 (6), pp.2164-2168. ⟨10.1021/acs.orglett.1c00321⟩. ⟨hal-03416913⟩