A copper-catalyzed annulation of
3-aryl-2H-azirines
with 2-naphthols has been developed for the rapid assembly of C-3-naphthol-substituted
benzo[e]indoles in one pot. This cascade reaction
was realized through dearomatic nucleophilic ring opening of azirine,
intramolecular cyclization, and oxidative cross-dehydrogenative coupling
to furnish the important unreported π-expanded naphthol/benzo[e]indole biaryls.