Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 15, Issue 37, Pages 7898-7908Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7ob01889d
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Funding
- National Key Research and Development Program of China [2016YFA0602900]
- National Natural Science Foundation of China [21502055, 21490572, 21672072]
- Fundamental Research Funds for the Central Universities [2015ZY001, 2015ZM150]
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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.
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