반응 #652871

ord-558a614df4b24cec91e6fce11bd56a62

반응 조건

온도
180°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타The organic layer was separated
  2. 2
    추출the aqueous layer was extracted with ethyl acetate
  3. 3
    세척The pooled organic layer was washed with water and saturated aqueous NaCl
  4. 4
    건조dried over MgSO4
  5. 5
    여과filtered
  6. 6
    농축concentrated under reduced pressure
  7. 7
    기타To a solution prepared
  8. 8
    추출extracted with 3 portions of ethyl acetate
  9. 9
    세척The pooled organic layer was washed with water and saturated aqueous NaCl
  10. 10
    건조dried over MgSO4
  11. 11
    여과filtered
  12. 12
    농축the filtrate was concentrated under reduced pressure
  13. 13
    기타recrystallized from ethyl acetate/hexane

실험 절차

In ethyl acetate was suspended 2.0 g of 4-benzyloxypiperidine hydrochloride and the suspension was neutralized with aqueous 1N-auqeous sodium hydroxide. The organic layer was separated and the aqueous layer was extracted with ethyl acetate. The pooled organic layer was washed with water and saturated aqueous NaCl, dried over MgSO4, filtered, and concentrated under reduced pressure. To a solution prepared by dissolving the resulting 4-benzyloxypiperidine in 0.5 mL of toluene were added 1.1 g of 2-bromomethyl-2,3-dihydro-2,4,6,7-tetramethyl-5-benzofuranamine and 2.8 mL of triethylamine, and in an autoclave, the mixture was stirred under nitrogen gas at 180° C. for 15 hours. This reaction mixture was diluted with saturated aqueous NaHCO3 and extracted with 3 portions of ethyl acetate. The pooled organic layer was washed with water and saturated aqueous NaCl, dried over MgSO4, and filtered and the filtrate was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography (hexane/ethyl acetate=1:1) and recrystallized from ethyl acetate/hexane to provide 1.1 g of the title compound. Yield 67%.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US06172085B2uspto-grants-2001_01