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Issue 12, 2012
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One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation

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Abstract

The reaction of readily accessible 1,1-dialkylhydrazones with commercially available o-(trimethylsilyl)aryl triflates provides a direct one-step route to pharmaceutically important 1-alkylindazoles. The products are obtained in high yields by one-pot NCS-chlorination/aryne annulation or Ac2O-acylation/deprotection/aromatization protocols.

Graphical abstract: One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation

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Publication details

The article was received on 16 Dec 2011, accepted on 16 Jan 2012 and first published on 17 Jan 2012


Article type: Paper
DOI: 10.1039/C2OB07117G
Citation: Org. Biomol. Chem., 2012,10, 2409-2412
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    One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation

    N. A. Markina, A. V. Dubrovskiy and R. C. Larock, Org. Biomol. Chem., 2012, 10, 2409
    DOI: 10.1039/C2OB07117G

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