反応 #7939

ord-adef68c798704d7e9c50dde96c01cffe

反応条件

温度
90°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他was purged with nitrogen
  2. 2
    その他The resulting mixture was purged with nitrogen
  3. 3
    温度After cooling
  4. 4
    その他the solvent was evaporated under vacuum
  5. 5
    洗浄The residue in EtOAc (10 mL) was washed with water (2×5 mL) and brine (5 ml)
  6. 6
    乾燥dried over MgSO4
  7. 7
    ろ過filtered
  8. 8
    その他evaporated under vacuum to a gum (194 mg)
  9. 9
    その他The crude product was purified by preparative layer chromatography (PLC) on two 0.1×20×20 cm silica gel GF plates
  10. 10
    洗浄The major UV visible band at Rf 0.15-0.25 was eluted with EtOAc
  11. 11
    その他the solvent evaporated under vacuum

実験手順

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.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07087599B2uspto-grants-2006_08