반응 #342117

ord-3d0f3b3a5d104fabbe96ee66cebd9ef1

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도heated
  2. 2
    온도at reflux
  3. 3
    기타irradiated with light (100 W bulb) for 4 hours
  4. 4
    여과The reaction mixture was filtered
  5. 5
    농축concentrated
  6. 6
    workup.DISSOLUTIONThe residue was dissolved in THF (50 mL)
  7. 7
    여과filtered
  8. 8
    기타The solvent of the filtrate was evaporated
  9. 9
    기타The bright orange residue obtained
  10. 10
    추출extracted with ethyl acetate (2×25 mL)
  11. 11
    추출extracted with methylene chloride
  12. 12
    건조Both ethyl acetate solution and methylene chloride solution were dried over anhydrous Na2SO4 separately
  13. 13
    기타Evaporation of ethyl acetate solution
  14. 14
    기타afforded an orange oil which
  15. 15
    기타was recrystallized from hexane

실험 절차

5-Fluoro-2-nitrotoluene (1.55 g, 10 mmol), N-bromosuccinimide (1.82 g, 10 mmol), and benzoyl peroxide (0.1 g, 0.4 mmol) were dissolved in CCl4 (50 mL), heated at reflux, and irradiated with light (100 W bulb) for 4 hours. The reaction mixture was filtered and concentrated. The residue was dissolved in THF (50 mL). Morpholine (1.9 g, 22 mmol) was added to the THF solution. The mixture was stirred at ambient temperature for 1 hour and then filtered. The solvent of the filtrate was evaporated. The bright orange residue obtained was then mixed with 5% HCl solution (30 mL) and extracted with ethyl acetate (2×25 mL). The aqueous layer was basified with NaOH solution to pH 8 and then extracted with methylene chloride. Both ethyl acetate solution and methylene chloride solution were dried over anhydrous Na2SO4 separately. Evaporation of ethyl acetate solution afforded an orange oil which was recrystallized from hexane:ether solution to yield 450 mg of a yellow solid, 4-(3-methyl-4-nitrophenyl)morpholine (18%), the by-product. Evaporation of methylene chloride solution afforded 660 mg of the desired compound, 4-(5-fluoro-2-nitrobenzyl)morpholine (27.5%).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07875728B2uspto-grants-2011_01