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Palladium-Catalyzed Synthesis of 2-(Aminomethyl)indoles from Ethyl 3-(o-Trifluoroacetamidophenyl)-1-propargyl Carbonate

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journal contribution
posted on 11.05.2006, 00:00 by Ilaria Ambrogio, Sandro Cacchi, Giancarlo Fabrizi
The palladium-catalyzed reaction of ethyl 3-(o-trifluoroacetamidophenyl)-1-propargyl carbonate with piperazines in the presence of Pd(PPh3)4 in THF at 80 °C affords 2-(piperazin-1-ylmethyl)indoles in excellent yields. Good to excellent yields are also obtained with other secondary amines.