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Synlett 2011(5): 623-626  
DOI: 10.1055/s-0030-1259548
LETTER
© Georg Thieme Verlag Stuttgart ˙ New York

Domino Ligand-Free Copper-Catalyzed Synthesis of Polysubstituted Indoles

Md Ashif Ali, Tharmalingam Punniyamurthy*
Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati 781039, India
Fax: +91(361)2690762; e-Mail: tpunni@iitg.ernet.in;
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Publication History

Received 24 September 2010
Publication Date:
11 February 2011 (online)

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Abstract

The synthesis of polysubstituted indoles is described by the domino reaction of 2-haloanilines and 1,3-dicarbonyl compounds, 1,3-diketones, β-keto esters and β-keto amides, using copper catalysis under ligand-free conditions. The protocol provides a simple, general and atom economical process for the synthesis of substituted indoles at moderate temperature.

Key words

Cu2O - indoles - cesium carbonate - 1,3-dicarbonyl compounds - 2-haloanilines

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