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Issue 17, 2010
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Synthesis of 4-functionalized-1H-indoles from 2,3-dihalophenols

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Abstract

A new synthesis of 4-halo-1H-indoles has been developed from easily available 2,3-dihalophenol derivatives. The key steps are Smiles rearrangement and a one-pot or stepwise Sonogashira coupling/NaOH-mediated cyclization. Subsequent functionalization allows access to a wide variety of 2,4- or 2,3,4-regioselectively functionalized indoles.

Graphical abstract: Synthesis of 4-functionalized-1H-indoles from 2,3-dihalophenols

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Publication details

The article was received on 17 Mar 2010, accepted on 21 Jun 2010 and first published on 08 Jul 2010


Article type: Communication
DOI: 10.1039/C004360E
Citation: Org. Biomol. Chem., 2010,8, 3860-3864

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    Synthesis of 4-functionalized-1H-indoles from 2,3-dihalophenols

    R. Sanz, V. Guilarte and N. García, Org. Biomol. Chem., 2010, 8, 3860
    DOI: 10.1039/C004360E

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