Synthesis of a library of 2-alkyl-3-alkyloxy-2H-indazole-6-carboxamides

J Comb Chem. 2007 Jan-Feb;9(1):171-7. doi: 10.1021/cc060109o.

Abstract

A library of 200 2-alkyl-3-alkyloxy-2H-indazole-6-carboxamides was synthesized using parallel solution-phase methods. The indazole cyclization reaction was optimized for library production with the best yields resulting from controlled alcohol/water solvent ratios. The key step, a heterocyclization reaction, proceeds by N,N-bond formation and delivers the 2H-indazole scaffold. Automated preparative HPLC was utilized to provide pure compounds on a 10+ mg scale.

Publication types

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

MeSH terms

  • Amides / chemical synthesis*
  • Chromatography, Liquid
  • Combinatorial Chemistry Techniques / methods
  • Indazoles / chemical synthesis*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Structure
  • Nitrobenzoates / chemistry*

Substances

  • Amides
  • Indazoles
  • Nitrobenzoates
  • 4-bromomethyl-3-nitrobenzoic acid