Preparation of substituted piperazinones via tandem reductive amination-(N,N'-acyl transfer)-cyclization

Org Lett. 2002 Apr 4;4(7):1201-4. doi: 10.1021/ol025644l.


[reaction: see text] A one-pot, tandem reductive amination-transamidation-cyclization reaction was employed to produce substituted piperazin-2-ones in good yields. Various amino acid methyl esters and transferable acyl groups were examined to establish the reaction's scope.

MeSH terms

  • Amination
  • Cyclization
  • Models, Molecular
  • Molecular Conformation
  • Oxidation-Reduction
  • Piperazines / chemical synthesis*


  • Piperazines