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

Org Biomol Chem. 2012 Mar 28;10(12):2409-12. doi: 10.1039/c2ob07117g. Epub 2012 Feb 16.

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 Ac(2)O-acylation/deprotection/aromatization protocols.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Alkylation
  • Cyclization
  • Hydrazones / chemistry*
  • Indazoles / chemical synthesis*
  • Molecular Structure

Substances

  • Hydrazones
  • Indazoles