반응 #1862950

ord-e863dc89757a44acaa1705ec2e49005c

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    추출the resulting mixture was extracted with ethyl acetate
  2. 2
    건조The organic layer was dried over sodium sulfate
  3. 3
    기타the solvent was evaporated under reduced pressure
  4. 4
    workup.STIRRINGthe resulting mixture was stirred at 50° C. for 2.5 hours
  5. 5
    온도The reaction mixture was cooled to room temperature
  6. 6
    추출the resulting mixture was extracted with ethyl acetate
  7. 7
    건조The organic layer was dried over sodium sulfate
  8. 8
    기타the solvent was evaporated under reduced pressure
  9. 9
    기타The resulting residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=0/100 to 30/70)

실험 절차

(Step 1) To (S)-3-hydroxydihydrofuran-2(3H)-one (0.5 mL, 6.41 mmol), dichloromethane (6.4 mL), triethylamine (1.34 mL, 9.62 mmol), tert-butyldimethylsilylchloride (1.06 g, 7.07 mmol), and DMAP (39 mg, 0.321 mmol) were added, and the resulting mixture was stirred at room temperature for 3 hours. To the reaction mixture, a saturated aqueous ammonium chloride solution was added, and the resulting mixture was extracted with ethyl acetate. The organic layer was dried over sodium sulfate, and the solvent was evaporated under reduced pressure. To the obtained residue, methanol (11 mL) and sodium methoxide (331 mg, 6.13 mmol) were added, and the resulting mixture was stirred at 50° C. for 2.5 hours. The reaction mixture was cooled to room temperature, and a saturated aqueous ammonium chloride solution was added thereto, and then, the resulting mixture was extracted with ethyl acetate. The organic layer was dried over sodium sulfate, and the solvent was evaporated under reduced pressure. The resulting residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=0/100 to 30/70), whereby methyl (S)-2-(tert-butyldimethylsiloxy)-4-hydroxybutanoate (225 mg, 14%) was obtained.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09260459B2uspto-grants-2016_02