反応 #310616

ord-45054b6002454d509711c87a55c276dc

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    抽出the mixture was extracted with ether (x2)
  2. 2
    洗浄The extract was washed with water (x2)
  3. 3
    その他dried
  4. 4
    その他evaporated
  5. 5
    その他to leave a froth which
  6. 6
    洗浄the mixture was washed with ether (x2)
  7. 7
    抽出The wash was extracted with 2M-HCl solution
  8. 8
    抽出The mixture was extracted with ether (x2)
  9. 9
    洗浄the extract was washed with water (x2)
  10. 10
    その他dried
  11. 11
    その他evaporated
  12. 12
    その他to leave a froth which
  13. 13
    その他was purified by column chromatography
  14. 14
    洗浄eluted with CHCl3 :MeOH (9:1)

実験手順

A solution of 11α-amino-2β-ethoxy-3α-hydroxy-5α-pregnan-20-one 20-ethylene acetal (2 g) in ethanol (20 ml) was stirred with cyclohexanone (1.5 ml) and sodium cyanoborohydride (2.015 g) for 6 h. 5% NaHCO3 solution (40 ml) was added and the mixture was extracted with ether (x2). The extract was washed with water (x2), dried and evaporated to leave a froth which was dissolved in 2M-HCl solution (50 ml) and ethanol (50 ml). Water (100 ml) was added and the mixture was washed with ether (x2). The wash was extracted with 2M-HCl solution and the combined acid fraction was brought to basic pH with 2M-NaOH solution. The mixture was extracted with ether (x2) and the extract was washed with water (x2), dried and evaporated to leave a froth which was purified by column chromatography eluted with CHCl3 :MeOH (9:1) to give the title compound (1.235 g), [α]D +39°. νmax 1695 cm-1.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US04353898uspto-grants-1982_10