Organic letters

2-Aryl and 2-heteroaryl indoles from 1-alkynes and o-iodotrifluoroacetanilide through a domino copper-catalyzed coupling-cyclization process

S Cacchi, G Fabrizi, LM Parisi

Index: Cacchi, Sandro; Fabrizi, Giancarlo; Parisi, Luca M. Organic Letters, 2003 , vol. 5, # 21 p. 3843 - 3846

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Citation Number: 190

Abstract

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)(PPh3) 2] NO3 in the presence of K3PO4 in toluene or dioxane at 110° C. 2-Aryl and 2-heteroaryl indoles can also be isolated in good yields by using catalysts derived from CuI and PPh3 in dioxane at 110° C.