반응 #323285

ord-e483341d2f2b4e9e9ee294905738e732

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타was quenched in 1 liter of dilute sodium hydroxide
  2. 2
    추출The mixture was extracted with several portions of methylene chloride
  3. 3
    추출The combined methylene chloride extract
  4. 4
    세척was washed with several portions of 1M sodium hydroxide
  5. 5
    건조dried over magnesium sulfate
  6. 6
    기타evaporated in vacuo
  7. 7
    기타to give an oil which
  8. 8
    온도was refluxed for 1.5 hr
  9. 9
    기타The reaction mixture was quenched in ice water
  10. 10
    추출extracted with several portions of methylene chloride
  11. 11
    추출The combined methylene chloride extract
  12. 12
    건조was dried over magnesium sulfate
  13. 13
    기타evaporated in vacuo
  14. 14
    기타to give an oil

실험 절차

A solution of 51.13 g (0.125 mole) of 3-phenylsulfonic acid ester with 1-[(4-methylbenzene)sulfonyl)-3-piperidinol, 25.2 g (0.175 mole) of o-chlorothiophenol and 58 g of sodium carbonate in dimethylformamide was heated at 100° C. for 19 hr and then was quenched in 1 liter of dilute sodium hydroxide. The mixture was extracted with several portions of methylene chloride. The combined methylene chloride extract was washed with several portions of 1M sodium hydroxide, dried over magnesium sulfate and evaporated in vacuo to give an oil which was shown by NMR and mass spectroscopy to be N-tosyl-3-(o-chlorothiophenoxy)piperidine. A mixture of the oil and excess phenol in 200 ml of 48% hydrobromic acid was refluxed for 1.5 hr. The reaction mixture was quenched in ice water, made basic with sodium hydroxide and extracted with several portions of methylene chloride. The combined methylene chloride extract was dried over magnesium sulfate and evaporated in vacuo to give an oil, the free base of the title compound. The free base was converted to the hydrobromic acid salt which was recrystallized from isopropanol-acetonitrile-isopropyl ether, m.p. 152.5°-154.5° C.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US04642348uspto-grants-1987_02