Regio‐ and Stereoselective Construction of Highly Functionalized 3‐Benzazepine Skeletons through Ring‐Opening Cycloamination Reactions Catalyzed by Gold

Abstract

Ring size under control: Highly functionalized 1-amino- or 1-hydroxy-1H-benzo[d]azepines have been prepared through a gold-catalyzed cyclization of (o-alkynyl)phenyl aziridines with heteronucleophiles. After removal of the phthalimido group, the products can be further transformed into 1H-benzo[d]azepin-1-ones (see scheme; IBX=2-iodoxybenzoic acid, Phth=pthalimido).