반응 #1482265

ord-496eb5f43ab3414587bd1e77fa6074e6

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도under reflux for an additional hour
  2. 2
    온도To this Grignard solution, cooled down to 0°
  3. 3
    온도under reflux for 15 minutes
  4. 4
    온도the reaction mixture was cooled down to 0°
  5. 5
    추출extracted with a total of 0.5 l of ether
  6. 6
    세척The organic phase was washed neutral with water
  7. 7
    건조dried over magnesium sulfate
  8. 8
    기타After removal of the solvent
  9. 9
    기타on a rotary evaporator
  10. 10
    기타drying of the residue in a high vacuum
  11. 11
    기타there were obtained 10.5 g of a highly viscous oil, which
  12. 12
    기타for purification
  13. 13
    기타was chromatographed on 450 g of Kieselgel with ether/hexane/acetic ester (4:4:1 parts by volume)
  14. 14
    기타[α]D20 =-5.5° (c=1.20; CHCl3)

실험 절차

To 0.8 g of magnesium shavings activated with methyl iodide was added dropwise a solution of 7.77 g of 1-bromo-2,5-dimethoxy-3,4,6-trimethylbenzene in 20 ml of absolute tetrahydrofuran at a rate such that the solvent was brought just to boiling. Subsequently, the reaction mixture was boiled under reflux for an additional hour. To this Grignard solution, cooled down to 0°, were added dropwise 5.0 g of (S)-2,2,4-trimethyl-1,3-dioxolan-4-acetaldehyde. Subsequently, the reaction mixture was stirred at room temperature for a further 4 hours and under reflux for 15 minutes. For the working-up, the reaction mixture was cooled down to 0°, it was treated with 10 ml of saturated ammonium chloride solution followed by 10 ml of 2-N sulfuric acid and extracted with a total of 0.5 l of ether. The organic phase was washed neutral with water and dried over magnesium sulfate. After removal of the solvent on a rotary evaporator and drying of the residue in a high vacuum, there were obtained 10.5 g of a highly viscous oil, which, for purification, was chromatographed on 450 g of Kieselgel with ether/hexane/acetic ester (4:4:1 parts by volume). The yield of α-(2,5-dimethoxy-3,4,6-trimethylphenyl)-2,2,4-(S)-trimethyl-1,3-dioxolan-4-ethanol amounted to 8.83 g; [α]D20 =-5.5° (c=1.20; CHCl3).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US04201879uspto-grants-1980_05