反应详情

23.73 g (0.1 mole) of 2-amino-9-(4-hydroxy-3-(hydroxymethyl)but-1-yl)purine was suspended in 300 ml of tetrahydrofuran. To the suspension, 24.52 g (0.31 mole) of pyridine, 1.22 g (0.01 mole) of 4-dimethylaminopyridine and 21.44 g (0.21 mole) of acetic acid anhydride were added, and the mixture was stirred for five hours at room temperature. After completion of the reaction, the reaction product was concentrated under reduced pressure. The remaining concentrate was added to 300 ml of purified water and then extracted four times with 400 ml portions of chloroform. The organic layer was collected, and dried with anhydrous magnesium sulfate, followed by filtration and washing. The resulting filtrate was concentrated under reduced pressure and crystallized from butanol, thereby giving 24.10 g (75% yield) of white 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl-2-aminopurine (famciclovir).

1. customAfter completion of the reaction
2. concentrationthe reaction product was concentrated under reduced pressure
3. concentrationThe remaining concentrate
4. additionwas added to 300 ml of purified water
5. extractionextracted four times with 400 ml portions of chloroform
6. customThe organic layer was collected
7. dry with materialdried with anhydrous magnesium sulfate
8. filtrationfollowed by filtration
9. washwashing
10. concentrationThe resulting filtrate was concentrated under reduced pressure
11. customcrystallized from butanol