Copper-catalyzed [3+2] annulation of propargylic acetates with anilines in the presence of trimethylsilyl chloride leading to 2,3-disubstituted indoles via an aza-Claisen rearrangement

Abstract Described herein is the use of copper triflate to efficiently catalyze a [3+2] annulation of propargylic acetates with N -alkylanilines in the presence of trimethylsilyl chloride (Me 3 SiCl) to produce 2,3-disubstituted indole derivatives. Also, the copper(II) catalyst efficiently promoted an aza-Claisen rearrangement of N -arylated propargylic amines involving a 3-aza-1,5-enyne skeleton.