Aminofluorination of 2-alkynylanilines: A Au-catalyzed entry to fluorinated indoles

Abstract

The scope and limitations of gold-catalyzed tandem cycloisomerization/ fluorination reactions of unprotected 2-alkynylanilines to have access to 3,3-difluoro-2-aryl-3H-indoles and 3-fluoro-2-arylindoles are described. An unprecedented aminoauration/oxidation/ fluorination cascade reaction of 2-alkynylanilines bearing a linear alkyl group on the terminal triple bond is reported. © 2014 Arcadi et al; licensee Beilstein-Institut.