Rh(III)-catalyzed intermolecular C-H amination of 1-aryl-1H-pyrazol-5(4H)-ones with alkylamines

Org Lett. 2014 Jan 3;16(1):42-5. doi: 10.1021/ol402965d. Epub 2013 Dec 12.

Abstract

An intermolecular C-H amination of 1-aryl-1H-pyrazol-5(4H)-ones was achieved under mild reaction conditions, using a low catalyst loading and with a broad scope of aminating reagents. This protocol not only provides the first example of rhodium(III)-catalyzed intermolecular aromatic C-H amination directed by an intrinsic functionality of the substrate/product but also features aminating an existing drug with either primary or secondary N-benzoate alkylamines as the coupling partners.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amination
  • Amines / chemistry*
  • Catalysis
  • Molecular Structure
  • Organometallic Compounds / chemistry*
  • Pyrazolones / chemistry*
  • Rhodium / chemistry*

Substances

  • Amines
  • Organometallic Compounds
  • Pyrazolones
  • Rhodium