반응 #92314

ord-fb3e8ce4f8454649be1829394b18c905

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도had been cooled on ice
  2. 2
    기타to separate it
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    추출The aqueous layer was extracted with ethyl acetate (50 ml)
  4. 4
    세척were then washed with a 5% citric acid aqueous solution (40 ml)
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    세척The resulting organic layer was washed with saturated saline (30 ml)
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    농축was then concentrated under reduced pressure
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    workup.ADDITIONThereafter, isopropyl alcohol (50 ml) was added to the residue
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    농축the solvent was then concentrated under reduced pressure, so that the volume
  9. 9
    온도The obtained slurry liquid was cooled to −10° C.
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    여과a precipitate was filtered
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    세척was then washed with ice-
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    온도cooled isopropyl alcohol (10 ml)

실험 절차

Under a nitrogen atmosphere, 1,3-dibromo-5,5-dimethylhydantoin (4) (11.6 g, 40.6 mol) was added to a solution of (S)-3-cyclohexene-1-carboxylic acid (R)-α-phenylethylamine salt (2-b) (10.0 g, 40.4 mmol) in acetonitrile (25 ml) that had been cooled on ice. The temperature of the reaction solution was increased to room temperature, and the reaction solution was then stirred for 2 hours. Thereafter, ethyl acetate (50 ml) and a 10% sodium thiosulfate aqueous solution (40 ml) were added to the reaction solution to separate it. The aqueous layer was extracted with ethyl acetate (50 ml), and the organic layers were gathered and were then washed with a 5% citric acid aqueous solution (40 ml). The resulting organic layer was washed with saturated saline (30 ml) and was then concentrated under reduced pressure. Thereafter, isopropyl alcohol (50 ml) was added to the residue, and the solvent was then concentrated under reduced pressure, so that the volume became 30 ml. The obtained slurry liquid was cooled to −10° C., and a precipitate was filtered and was then washed with ice-cooled isopropyl alcohol (10 ml) to obtain the title compound (6.9 g, yield: 84%).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09447118B2uspto-grants-2016_09