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Issue 31, 2016
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Palladium-catalysed direct C-2 methylation of indoles

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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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Supplementary files

Article information


Submitted
14 Jun 2016
Accepted
07 Jul 2016
First published
07 Jul 2016

Org. Biomol. Chem., 2016,14, 7443-7446
Article type
Communication

Palladium-catalysed direct C-2 methylation of indoles

D. Tu, X. Cheng, Y. Gao, P. Yang, Y. Ding and C. Jiang, Org. Biomol. Chem., 2016, 14, 7443
DOI: 10.1039/C6OB01281G

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