De novo synthesis of polysubstituted β-naphthylamines via Tf2O-mediated [4+2] annulation of amides with alkynes

A conceptually new strategy has been described for the mild and environmentally friendly preparation of β-naphthylamines via Tf2O-activated cyclization of amides with alkynes. Both terminal and internal alkynes could serve as effective nucleophiles in this transformation. This chemistry features simple reaction conditions, high chemoselectivities, wide substrate scope, and offers a practical approach to polysubstituted β-naphthylamines.