반응 #700932

ord-681f1ea58dc9427f8dfadf5d9d5628db

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.STIRRINGstirring
  2. 2
    workup.WAITcontinued for 18 hours
  3. 3
    온도was cooled in ice
  4. 4
    기타The organic layer was separated
  5. 5
    추출the aqueous extracted with ethyl acetate
  6. 6
    세척The combined organic extracts were washed with brine
  7. 7
    건조dried (MgSO4)
  8. 8
    기타The solvent was removed in vacuo
  9. 9
    기타to give a pale yellow oil
  10. 10
    온도the mixture was heated
  11. 11
    온도at reflux for 1 hour
  12. 12
    기타The volatiles were removed in vacuo
  13. 13
    세척washed with ethyl acetate
  14. 14
    추출extracted with ethyl acetate
  15. 15
    세척this ethyl acetate was washed with water
  16. 16
    건조dried (MgSO4)
  17. 17
    기타the volatiles removed in vacuo

실험 절차

2-(4Chlorophenyl)ethanol (10 g) was stirred in 50% aqueous sodium hydroxide (70 ml), tetrabutylammoniumbromide (1.4 g) was added and the mixture stirred for 1 hour. t-Butylbromoacetate (28.6 ml) in toluene (140 ml) was added and stirring continued for 18 hours. Water (50 ml) was added and after 2 hours the mixture was cooled in ice and acidified to pH 1 with concentrated hydrochloric acid. The organic layer was separated and the aqueous extracted with ethyl acetate. The combined organic extracts were washed with brine and dried (MgSO4). The solvent was removed in vacuo to give a pale yellow oil This was dissolved in dichoromethane (100 ml) and trifluoroacetic acid (100 ml) added, the mixture was heated at reflux for 1 hour. The volatiles were removed in vacuo and the residue taken up in sodium hydroxide and washed with ethyl acetate. The aqueous layer was then acidified with concentrated hydrochloric acid and extracted with ethyl acetate, this ethyl acetate was washed with water, dried (MgSO4) and the volatiles removed in vacuo to provide the subtitle compound as a buff solid (16.4 g) which was used without further purification.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US06008365uspto-grants-1999_12