Preparation of fluoroalkyl imines, amines, enamines, ketones, alpha-amino carbonyls, and alpha-amino acids from primary enamine phosphonates

J Org Chem. 2004 Dec 10;69(25):8767-74. doi: 10.1021/jo048682m.

Abstract

A simple method for preparation of fluoroalkyl beta-enaminophosphonates 1 from alkylphosphonates 2 and perfluoroalkyl nitriles 3 is reported. Olefination reaction of functionalized phosphates 1 with aldehydes gives alpha,beta-unsaturated imines 5. Acid hydrolysis of these fluoroalkyl derivatives 5 affords alpha,beta-unsaturated ketones 6, while their selective reduction with hydrides leads to the formation of allylamines 7, enamines 8, and saturated ketones 9 or amines 10. Selective oxidative cleavage of the carbon-carbon double bond of allylamines 7 gives fluorinated alpha-amino aldehydes 12, alpha-amino ketones 13, or alpha-amino acid derivatives 14.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetaldehyde / chemical synthesis*
  • Amines* / chemical synthesis
  • Amines* / chemistry
  • Amino Acids / chemical synthesis*
  • Imines / chemical synthesis*
  • Ketones / chemical synthesis*
  • Molecular Structure
  • Organophosphonates / chemistry*

Substances

  • Amines
  • Amino Acids
  • Imines
  • Ketones
  • Organophosphonates
  • Acetaldehyde