Palladium-catalysed direct C-2 methylation of indoles†
Daoquan Tu,Xiuzhi Cheng,Yadong Gao,Panpan Yang,Yousong Ding,Chao Jiang
Organic & Biomolecular Chemistry Pub Date : 07/07/2016 00:00:00 , DOI:10.1039/C6OB01281G
Abstract

A direct C-2 methylation reaction of indoles bearing a readily removable N-2-pyrimidyl moiety as a site-specific directing group has been developed with a palladium catalyst. This reaction relied on the use of KF to promote efficient methylation. A moderate to good yield was achieved in a range of indole substrates.

Graphical abstract: Palladium-catalysed direct C-2 methylation of indoles