Abstract
We have developed a simple and efficient method for the arylation of 3-(aminoalkyl)indoles with aryl alcohols and other aromatic nucleophiles through C–N bond cleavage under microwave irradiation to synthesize 3-(α,α-diarylmethyl)indoles. The method uses thiourea as catalyst, which is environmentally benign, water-tolerant and easy to handle. Notably, acid-sensitive substrates are tolerated under the reaction conditions. Thiourea activates the tertiary amine through double hydrogen bonding and converts it into a better leaving group. The reaction proceeds through the formation of vinylogous iminium ion as an intermediate.
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