Concepedia

Palladium-catalysed direct C-2 methylation of indoles

Daoquan Tu, Xiuzhi Cheng, Yadong Gao, Panpan Yang, Yousong Ding, Chao Jiang

Organic & Biomolecular Chemistry · 2016 · 25 citations · 47 references

DOI

Concepts

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.

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