反応 #46289

ord-3bbc7e5ac5a74798ab3ef4002e1dcdfe

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    洗浄The product mixture was washed successively with aqueous NaHCO3, water, and brine
  2. 2
    抽出The organic extract
  3. 3
    乾燥was dried over anhydrous sodium sulfate
  4. 4
    ろ過filtered
  5. 5
    濃縮concentrated under vacuum
  6. 6
    その他This intermediate silylated aminoalcohol was used without further purification
  7. 7
    濃縮The reaction mixture was concentrated under vacuum
  8. 8
    その他The residue was partitioned between ethyl acetate and aqueous sodium carbonate
  9. 9
    抽出The organic extract
  10. 10
    乾燥was dried over anhydrous sodium sulfate
  11. 11
    ろ過filtered
  12. 12
    濃縮concentrated under vacuum
  13. 13
    その他Collection and concentration of appropriate fractions

実験手順

A mixture of 4-hydroxybutylamine (4.0 g, 44.9 mmol), tert-butyldimethyl-silyl chloride (7.4 g, 49.3 mmol) and imidazole (6.7 g, 98.7 mmol) in dichloromethane (150 mL) was stirred at room temperature for 2 hours. The product mixture was washed successively with aqueous NaHCO3, water, and brine. The organic extract was dried over anhydrous sodium sulfate, filtered, and concentrated under vacuum. This intermediate silylated aminoalcohol was used without further purification. To a mixture of the amine (1.0 g, 4.9 mmol) and benzyloxyacetaldehyde (0.74 g, 4.9 mmol) in dichloroethane (15 mL) at room temperature, sodium triacetoxyborohydride (1.3 g, 6.3 mmol) was added. The reaction mixture was concentrated under vacuum. The residue was partitioned between ethyl acetate and aqueous sodium carbonate. The organic extract was dried over anhydrous sodium sulfate, filtered, and concentrated under vacuum. The residue was subjected to column chromatography on silica gel eluting with 2% methanol in dichloromethane. Collection and concentration of appropriate fractions afforded the title silyloxybutyl-amine.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07741315B2uspto-grants-2010_06