반응 #7939

ord-adef68c798704d7e9c50dde96c01cffe

반응 조건

온도
90°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타was purged with nitrogen
  2. 2
    기타The resulting mixture was purged with nitrogen
  3. 3
    온도After cooling
  4. 4
    기타the solvent was evaporated under vacuum
  5. 5
    세척The residue in EtOAc (10 mL) was washed with water (2×5 mL) and brine (5 ml)
  6. 6
    건조dried over MgSO4
  7. 7
    여과filtered
  8. 8
    기타evaporated under vacuum to a gum (194 mg)
  9. 9
    기타The crude product was purified by preparative layer chromatography (PLC) on two 0.1×20×20 cm silica gel GF plates
  10. 10
    세척The major UV visible band at Rf 0.15-0.25 was eluted with EtOAc
  11. 11
    기타the solvent evaporated under vacuum

실험 절차

A mixture of 9a-butyl-7-methoxy-4-[4-(trifluoromethane-sulfonyloxy)-phenyl]-1,2,9,9a-tetrahydro-3H-fluoren-3-one (98.9 mg, 0.2 mmol), methyl (E)-3-tributylstannyl-acrylate (112.5 mg, 0.3 mmol) and lithium chloride (25.4 mg, 0.6 mmol) in anhydrous dimethylformamide (1.0 mL) was purged with nitrogen and treated with bis(triphenylphosphine)palladium(II) chloride (7.0 mg, 0.01 mmol). The resulting mixture was purged with nitrogen then stirred under a nitrogen atmosphere with heating in an oil bath at 90° C. for 60 minutes. After cooling, the solvent was evaporated under vacuum. The residue in EtOAc (10 mL) was washed with water (2×5 mL) and brine (5 ml), dried over MgSO4, filtered, and evaporated under vacuum to a gum (194 mg). The crude product was purified by preparative layer chromatography (PLC) on two 0.1×20×20 cm silica gel GF plates, developing with 4:1-hexanes-EtOAc. The major UV visible band at Rf 0.15-0.25 was eluted with EtOAc and the solvent evaporated under vacuum to afford methyl (2E)-3-[4-(9a-butyl-7-methoxy-3-oxo-2,3,9,9a-tetrahydro-1H-fluoren-4-yl)phenyl]-2-propenoate (83 mg) as a pale yellow solid. NMR showed approximately 7-8% of a Bu3SnX impurity.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07087599B2uspto-grants-2006_08