反応 #61839

ord-0a8fbca072a041dca7231b7ad252d79e

反応条件

温度
115°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度under reflux for 4 hours
  2. 2
    温度The mixture was cooled
  3. 3
    その他evaporated in vacuo
  4. 4
    その他partitioned between dichloromethane and brine
  5. 5
    その他The organic layer was separated
  6. 6
    乾燥dried with sodium sulphate
  7. 7
    ろ過filtered
  8. 8
    その他evaporated in vacuo
  9. 9
    その他to afford
  10. 10
    温度under reflux for 96 hours
  11. 11
    温度After cooling the volatiles
  12. 12
    その他were removed in vacuo
  13. 13
    温度The mixture was cooled
  14. 14
    その他triturated with chloroform (80 ml)
  15. 15
    ろ過filtered
  16. 16
    洗浄The filtrate was washed with water
  17. 17
    乾燥dried with sodium sulphate
  18. 18
    ろ過filtered
  19. 19
    その他evaporated in vacuo

実験手順

A mixture of 2-acetoxy-3-methyl-1-(naphth-1-yl)butan-1-one (8.4 g), IMS (200 ml) and hydrochloric acid (1M; 100 ml) were boiled under reflux for 4 hours. The mixture was cooled, evaporated in vacuo and partitioned between dichloromethane and brine. The organic layer was separated, dried with sodium sulphate, filtered and evaporated in vacuo to afford a mixture of crude 2-hydroxy-3-methyl-1-naphthalen-1-yl-butan-1-one and 1-hydroxy-3-methyl-1-naphthalen-1-yl-butan-2-one (F) (7.4 g). Cyanamide (1.3 g) and anhydrous ethanol (50 ml) were added and the resulting mixture was boiled under reflux for 96 hours. After cooling the volatiles were removed in vacuo and the residue heated at 115° C. for a further 48 hours. The mixture was cooled, triturated with chloroform (80 ml) and filtered. The filtrate was washed with water, dried with sodium sulphate, filtered and evaporated in vacuo. The title compound (7) was obtained (0.26 g; m.p. 127-129° C.) following silica gel column chromatography of the residue in 33% ethyl acetate in petroleum ether and re-crystallisation from dichloromethane/petroleum ether.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07429607B2uspto-grants-2008_09