反応 #7955

ord-95e98eaea1a94f0591c92261b6aa3074

反応条件

温度
0°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    workup.ADDITIONwas added by syringe
  2. 2
    温度to slowly warm to room temperature
  3. 3
    workup.STIRRINGstirred at room temperature overnight
  4. 4
    抽出The aqueous phase was extracted with more EtOAc (20 mL)
  5. 5
    洗浄The combined organics were washed with 5% NaHCO3, water, and brine
  6. 6
    乾燥dried over MgSO4
  7. 7
    ろ過filtered
  8. 8
    濃縮concentrated under vacuum to a yellow oil
  9. 9
    その他The crude product was purified by preparative layer chromatography (PLC) on a 0.1×20×20 cm silica gel GF plate
  10. 10
    抽出The band at Rf 0.44-0.56 was extracted with EtOAc
  11. 11
    その他the extracts evaporated under vacuum

実験手順

A solution of 9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (162 mg, 0.52 mmol) in anhydrous THF (2.5 mL) was cooled in an ice bath and stirred under a nitrogen atmosphere while 0.4M LDA in THF (1.55 mL, 0.62 mmol) was added by syringe. After stirring at 0° C. for 30 minutes, the solution was cooled to −78° C. (dry ice-acetone bath) and treated with iodomethane (0.162 mL, 2.6 mmol). The resulting mixture was allowed to slowly warm to room temperature, then stirred at room temperature overnight. The mixture was diluted with EtOAc (60 mL) and shaken with saturated aqueous NH4Cl (40 mL). The aqueous phase was extracted with more EtOAc (20 mL). The combined organics were washed with 5% NaHCO3, water, and brine, dried over MgSO4, filtered, and concentrated under vacuum to a yellow oil. The crude product was purified by preparative layer chromatography (PLC) on a 0.1×20×20 cm silica gel GF plate using 4:1 hexanes-EtOAc as developing solvent. The band at Rf 0.44-0.56 was extracted with EtOAc and the extracts evaporated under vacuum to provide (2SR,9aSR)-9a-butyl-2,4-dimethyl-7-methoxymethoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (111 mg) as an oil.

出典

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