تفاعل #440807

ord-a9c8a9652cdc4e3fbcae8d09a886e04b

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    درجة الحرارةThe mixture was heated
  2. 2
    درجة الحرارةunder reflux for two hours
  3. 3
    أخرىthe solvent removed under reduced pressure
  4. 4
    درجة الحرارةThe resulting solution was heated
  5. 5
    درجة الحرارةunder reflux under a nitrogen atmosphere for 3 hours
  6. 6
    درجة الحرارةThe mixture was cooled to room temperature
  7. 7
    غسيلwashed with a saturated aqueous solution of sodium hydrogen carbonate
  8. 8
    أخرىThe organic layer was separated
  9. 9
    تجفيفdried over anhydrous magnesium sulphate
  10. 10
    ترشيحfiltered
  11. 11
    أخرىthe solvent removed under reduced pressure
  12. 12
    أخرىThe residue was purified by column chromatography on silica gel using gradient elution with ethyl acetate:pentane (70:30, by volume)

الإجراء التجريبي

A suspension of methyl 6-[(2,2-diphenylethyl)amino]-9H-purine-2-carboxylate (Preparation 7) (1.5 g, 4.02 mmol) in 1,1,1-trichloroethane (40 ml) was treated with N,O-bis(trimethylsilyl)acetamide (4.8 ml, 19.6 mmol). The mixture was heated under reflux for two hours. The solution was allowed to cool to room temperature and the solvent removed under reduced pressure. The residue was taken up in anhydrous toluene (40 ml) and 1,2,3,5-tetra-O-acetyl-β-D-ribofuranose (1.65 g, 5.19 mmol) and trimethylsilyl trifluoromethanesulfonate (0.98 ml, 5.43 mmol) added. The resulting solution was heated under reflux under a nitrogen atmosphere for 3 hours. The mixture was cooled to room temperature, diluted with ethyl acetate (200 ml) and washed with a saturated aqueous solution of sodium hydrogen carbonate. The organic layer was separated, dried over anhydrous magnesium sulphate, filtered and the solvent removed under reduced pressure. The residue was purified by column chromatography on silica gel using gradient elution with ethyl acetate:pentane (70:30, by volume) then ethyl acetate:pentane (80:20, by volume) then ethyl acetate to afford the title compound as a foam (2.05 g).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US06753322B2uspto-grants-2004_06