반응 #1477

ord-95296aadd2f34ea7a8a15d80c932bee0

용매

반응 조건

온도
-20°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타The reaction was quenched at 0° C. with saturated ammonium chloride solution (20 ml)
  2. 2
    추출extracted with EtOAc (2×50 ml)
  3. 3
    추출The combined extract
  4. 4
    세척was washed with water (20 ml), brine (20 ml)
  5. 5
    건조dried over MgSO4
  6. 6
    기타The solvent was evaporated under reduced pressure
  7. 7
    기타to afford a yellow oil
  8. 8
    기타The resultant reaction solution
  9. 9
    온도was heated in an oil bath (60° C.) for 3 h
  10. 10
    온도The reaction was cooled
  11. 11
    기타quenched with water (20 ml)
  12. 12
    추출extracted with EtOAc (2×50 ml)
  13. 13
    추출The combined extract
  14. 14
    세척was washed with saturated NaHCO3 (20 ml), water (20 ml), brine (20 ml)
  15. 15
    건조dried over MgSO4
  16. 16
    농축The solvent was concentrated in vacuo

실험 절차

In a flame dried round bottom flask 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound G, 2.0 g, 7.93 mmol) was dissolved in anhydrous THF (50 ml) and 3,4,5,6,-tetrahydro-2(H)-pyrimidinone (DMPU) (11.5 ml, 95.16 mmol) was added, under argon atmosphere. The reaction was then cooled to -20° C. and a solution of t-butyl magnesium chloride (16 ml, 31.7 mmol) (2M in Et2O) was added dropwise and stirred at -20° C. for 2 h and at ambient temperature for 1 h, under argon atmosphere. The reaction was quenched at 0° C. with saturated ammonium chloride solution (20 ml) and extracted with EtOAc (2×50 ml). The combined extract was washed with water (20 ml), brine (20 ml) and dried over MgSO4. The solvent was evaporated under reduced pressure to afford a yellow oil. To this yellow oil were added MeOH (50 ml) and p-tolylsulfonic acid (100 mg). The resultant reaction solution was heated in an oil bath (60° C.) for 3 h. The reaction was cooled and quenched with water (20 ml), extracted with EtOAc (2×50 ml). The combined extract was washed with saturated NaHCO3 (20 ml), water (20 ml), brine (20 ml), and dried over MgSO4. The solvent was concentrated in vacuo and the title compound was obtained as a colorless oil after purification by flash chromatography (silica, hexane).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05723666uspto-grants-1998_03