Preparation of substituted piperazinones via tandem reductive amination-(N,N'-acyl transfer)-cyclization.
[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.
Beshore
Douglas C
DC
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. douglas_beshore@merck.com
Dinsmore
Christopher J
CJ
D000586:Amination; D003500:Cyclization; D008958:Models, Molecular; D008968:Molecular Conformation; D010084:Oxidation-Reduction; D010879:Piperazines / Q000138:chemical synthesis*
D010879:Piperazines