Synthesis of o-(dimethylamino)aryl ketones, acridones, acridinium salts, and 1H-indazoles by the reaction of hydrazones and arynes

J Org Chem. 2012 Dec 21;77(24):11232-56. doi: 10.1021/jo302378w. Epub 2012 Dec 3.

Abstract

A novel, efficient route to biologically and pharmaceutically important o-(dimethylamino)aryl ketones, acridones, acridinium salts, and 1H-indazoles has been developed starting from readily available hydrazones of aldehydes and o-(trimethylsilyl)aryl triflates. The reaction proceeds through arynes under mild conditions, tolerates a wide range of functional groups, and provides the final products in good to excellent yields.

Publication types

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

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / chemistry
  • Acridones
  • Benzene Derivatives / chemistry*
  • Chemistry Techniques, Synthetic
  • Cyclization
  • Halogenation
  • Hydrazones / chemistry*
  • Imines / chemistry
  • Indazoles / chemical synthesis*
  • Indazoles / chemistry
  • Ketones / chemical synthesis*
  • Ketones / chemistry
  • Nitriles / chemistry
  • Salts / chemistry*

Substances

  • Acridines
  • Acridones
  • Benzene Derivatives
  • Hydrazones
  • Imines
  • Indazoles
  • Ketones
  • Nitriles
  • Salts
  • benzyne
  • ketimine
  • acridone