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Preparation of Substituted Piperazinones via Tandem Reductive Amination-(N,N'-Acyl Transfer)-Cyclization

Douglas C. Beshore* and Christopher J. Dinsmore

*Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, Email:

D. C. Beshore, C. J. Dinsmore, Org. Lett., 2002, 4, 1201-1204.

DOI: 10.1021/ol025644l


A one-pot, tandem reductive amination-transamidation-cyclization reaction produces substituted piperazin-2-ones in good yields.

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reaction pathway

Key Words

Reductive Amination, Transamidation, Sodium Triacetoxyborohydride

ID: J54-Y2002-880