반응 #7974

ord-7dd6343aeafb46f08ecf5adfe3390eb6

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도cooled in a dry ice-acetone bath
  2. 2
    workup.ADDITIONwas added by syringe
  3. 3
    기타The cooling bath was removed
  4. 4
    workup.ADDITIONdiluted with 0.2N HCl (5 mL) and EtOAc (10 mL)
  5. 5
    workup.STIRRINGshaken
  6. 6
    기타The organic phase was separated
  7. 7
    세척washed with brine
  8. 8
    건조dried over MgSO4
  9. 9
    여과filtered
  10. 10
    기타evaporated under vacuum to a solid (35.2 mg)
  11. 11
    기타The crude product was purified by flash chromatography on EM silica gel 60 (230-400 mesh, 1×18 cm column)
  12. 12
    세척as eluting solvent
  13. 13
    기타collecting 3 mL fractions
  14. 14
    농축concentrated under vacuum to approximately 1 mL of a suspension
  15. 15
    여과The suspension was filtered
  16. 16
    세척the solid portion washed with EtOAc
  17. 17
    기타dried under vacuum

실험 절차

A solution of (9SR,9aSR)-7-methoxy-4-methyl-9-propyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (38.3 mg, 0.142 mmol) in anhydrous CH2Cl2 (1.1 mL) was placed under a nitrogen atmosphere, cooled in a dry ice-acetone bath, and stirred while 1M BBr3 in CH2Cl2 (0.354 mL, 0.345 mmol) was added by syringe. The cooling bath was removed and the reaction mixture was stirred at room temperature for 2.6 hours, then diluted with 0.2N HCl (5 mL) and EtOAc (10 mL) and shaken. The organic phase was separated, washed with brine, dried over MgSO4, filtered, and evaporated under vacuum to a solid (35.2 mg). The crude product was purified by flash chromatography on EM silica gel 60 (230-400 mesh, 1×18 cm column) using 3:1 hexanes-EtOAc as eluting solvent, collecting 3 mL fractions. Fractions 12-26 were combined and concentrated under vacuum to approximately 1 mL of a suspension. The suspension was filtered and the solid portion washed with EtOAc and dried under vacuum to afford (9SR,9aSR)-7-hydroxy-4-methyl-9-propyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07087599B2uspto-grants-2006_08