Palladium-catalysed direct C-2 methylation of indoles?

Organic & Biomolecular Chemistry Pub Date: 2016-07-07 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
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