反应详情

Add 300 mg of palladium black to an argon-blanketed solution of 2600 mg (4.69 mmol) of 4-{[(3R)-1-benzylpiperidin-3-yl]oxy}-6-(2-fluorophenyl)-5-(4-methoxyphenyl)furo[2,3-d]-pyrimidine in 25 ml of a 4.4% solution of formic acid in methanol and stir at room temperature for five hours. Then add another 300 mg of palladium black and 0.9 ml of formic acid and stir at room temperature for a further 16 hours. After filtering off the catalyst, wash the catalyst residue with methanol/water. Concentrate the filtrate under reduced pressure, stir the residue in acetonitrile, filter off and dry under reduced pressure. 1376 mg (68% of theory) of the desired product are obtained.

1. stirringstir at room temperature for a further 16 hours
2. filtrationAfter filtering off the catalyst
3. washwash the catalyst residue with methanol/water
4. concentrationConcentrate the filtrate under reduced pressure
5. stirringstir the residue in acetonitrile
6. filtrationfilter off
7. customdry under reduced pressure