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N-Heterocyclic carbene palladium-catalyzed cascade annulation/alkynylation of 2-alkynylanilines with terminal alkynes

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Abstract

A straightforward and highly effective N-heterocyclic carbene-palladium catalyzed cascade annulation/alkynylation of 2-alkynylanilines with terminal alkynes has been enabled to afford free (NH)-3-alkynylindole derivatives in moderate to good yields. This protocol features mild conditions, broad substrate scope, and high atom- and step-economy. Notably, the resultant 3-alkynylindoles could be conveniently transformed into a variety of functionalized indole scaffolds, thus illustrating their potential applications in synthetic and pharmaceutical chemistry.

Graphical abstract: N-Heterocyclic carbene palladium-catalyzed cascade annulation/alkynylation of 2-alkynylanilines with terminal alkynes

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Publication details

The article was received on 30 Jul 2017, accepted on 01 Sep 2017 and first published on 01 Sep 2017


Article type: Paper
DOI: 10.1039/C7OB01889D
Citation: Org. Biomol. Chem., 2017, Advance Article
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    N-Heterocyclic carbene palladium-catalyzed cascade annulation/alkynylation of 2-alkynylanilines with terminal alkynes

    J. Li, C. Li, L. Ouyang, C. Li, W. Wu and H. Jiang, Org. Biomol. Chem., 2017, Advance Article , DOI: 10.1039/C7OB01889D

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