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Syntheses of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones: intermediates in the synthesis of aprepitant
Authors:Todd D. Nelson  Jonathan D. Rosen  Bridgette Craig  James M. McNamara
Affiliation:a Merck Research Laboratories, Department of Process Research, Merck & Co., 466 Devon Park Drive,Wayne, PA 19087, USA
b Merck Research Laboratories, Department of Process Research, 126 East Lincoln Avenue, Rahway, NJ 07065, USA
Abstract:The preparation of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones from N-substituted β-amino alcohols is reported. These were useful intermediates in the synthesis and development of aprepitant.
Keywords:Morpholine-3-ones   Morpholine-2,3-diones   Amino alcohols   Lactol   Lactam
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