Palladium-catalyzed synthesis of 2-(aminomethyl)indoles from ethyl 3-(o-trifluoroacetamidophenyl)-1-propargyl carbonate.
[reaction: see text] The palladium-catalyzed reaction of ethyl 3-(o-trifluoroacetamidophenyl)-1-propargyl carbonate with piperazines in the presence of Pd(PPh(3))(4) in THF at 80 degrees C affords 2-(piperazin-1-ylmethyl)indoles in excellent yields. Good to excellent yields are also obtained with other secondary amines.
Ambrogio
Ilaria
I
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università degli Studi La Sapienza, Roma, Italy.
Cacchi
Sandro
S
Fabrizi
Giancarlo
G