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Letter

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

Supporting Info

Douglas C. Beshore* and Christopher J. Dinsmore

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

Org. Lett., 2002, 4 (7), pp 1201–1204

DOI: 10.1021/ol025644l

Publication Date (Web): March 14, 2002

In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.

, douglas_beshore@merck.com

Abstract

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.

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Published In Issue April 04, 2002
Received January 30, 2002

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Letter

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