An efficient cascade methodology toward the synthesis of 2-substituted indoles has
been developed. The transformation proceeds via a palladium-catalyzed cross-coupling
reaction of o-nitrobenzyl cyanides with boronic acids. The use of Fe as co-catalyst during the
course of reaction employs significant enhancement in reaction rates. The developed
protocol allows for the unprecedented use of arylboronic acids as coupling partners
for constructing 2-substituted indoles.
Key words
cascade synthesis - 2-substituted indoles - palladium-catalyzed cross-coupling reaction