One-Pot Gold-Catalyzed Aminofluorination of Unprotected 2‑Alkynylanilines

Abstract

A tandem gold(I)-catalyzed aminocylization/fluorination and a two-step, one-pot gold(III)-catalyzed cyclization/electrophilic fluorination provide a convenient and general method for the synthesis of 3,3-difluoro-2-substituted-3<i>H</i>-indoles in good yield under mild conditions. Extension of the procedure to the synthesis of 2-aryl-3-fluoro-1<i>H</i>-indoles is described. The reaction proceeds smoothly in green ethanol and does not require any base, acid, or <i>N</i>-protective group