반응 #2713

ord-b76082d12d914f36b18aec03d29abfbc

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.STIRRINGthe mixture was stirred for 5 hours
  2. 2
    세척washed with brine (10 mL)
  3. 3
    기타dried
  4. 4
    기타the solvent was removed by evaporation
  5. 5
    기타to obtain the E and Z olefinic compounds, which
  6. 6
    온도cooled to -50° C
  7. 7
    온도The reaction mixture was gradually warmed to -10° C. over 3hours
  8. 8
    기타quenched with methanol and water
  9. 9
    workup.ADDITIONThe reaction mixture was diluted with ethyl acetate (100 mL)
  10. 10
    세척The organic layer was washed with brine
  11. 11
    기타dried
  12. 12
    기타Solvent was removed under reduced pressure
  13. 13
    기타the residue purified by chromatography on silicagel

실험 절차

To a cold (-78° C.) solution of ethyl 4-(diethoxyphosphoryl-3,3-dimethoxypropyl)benzoate (Compound D, 1.4 g, 3.6 mmol) in THF (9 mL) was added n-BuLi in hexane (1.6M solution, 2.8 mL). The mixture was gradually warmed to ambient temperature over 30 minutes and stirred for 5 minutes. To this mixture was added 2,2-dimethyl-4(tol-4-yl)-chrom-3-en-6-al (Compound Q, 260 mg, 0.93 mmol) in THF (1 mL) at ambient temperature and the mixture was stirred for 5 hours. The reaction mixture was diluted with ethyl acetate (100 mL) and washed with brine (10 mL) dried and the solvent was removed by evaporation. The residual material was subjected to flash chromatography on silicagel to obtain the E and Z olefinic compounds, which were dissolved in dichloromethane (5 mL) and cooled to -50° C. A solution of SnCl4 in dichloromethane (150 mg in 0.7 mL) was added to the olefinic compounds. The reaction mixture was gradually warmed to -10° C. over 3hours and then quenched with methanol and water. The reaction mixture was diluted with ethyl acetate (100 mL). The organic layer was washed with brine and dried. Solvent was removed under reduced pressure and the residue purified by chromatography on silicagel to afford the title compound as a white solid.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05728846uspto-grants-1998_03