Hypervalent iodine(III)-mediated benzannulation of enamines with alkynes for the synthesis of polysubstituted naphthalene derivatives.

A series of functionalized 1-amino-2-naphthalenecarboxylic acid derivatives were synthesized from enamines and alkynes via a benzannulation strategy mediated by iodosylbenzene and BF3·Et2O. The advantages of this novel benzannulation process include broad substrate scope, good functional group tolerance, and mild reaction conditions without the use of heavy metals.