2-Aryl and 2-Heteroaryl Indoles from 1-Alkynes and<i>o</i>-Iodotrifluoroacetanilide through a Domino Copper-Catalyzed Coupling−Cyclization Process

Abstract

[reaction: see text] A general method for the synthesis of 2-aryl and 2-heteroaryl indoles from aryl iodides and 1-alkynes through a domino copper-catalyzed process is reported. The best results have been obtained with [Cu(phen)(PPh(3))(2)]NO(3) in the presence of K(3)PO(4) in toluene or dioxane at 110 degrees C. 2-Aryl and 2-heteroaryl indoles can also be isolated in good yields by using catalysts derived from CuI and PPh(3) in dioxane at 110 degrees C.