反应详情

In a round bottom flask at room temperature was placed with 1.95 g (6.18 mmole) 1-benzyl-4-(5-fluoro-2-methoxy-phenyl)-4-hydroxypiperidine, (Intermediate 7) dry MeOH (40 mL), and the system purged with N2 for 5 min. To the solution, 1.95 g of 10% palladium on carbon was added. The system was again purged with N2 for 5 minutes followed by addition of 2 mL formic acid (88%). The resulting mixture was stirred at room temperature under N2 for one day. At this point, a further 2 mL of formic acid (88%) was added. The reaction was continued for 2.5 days. The mixture was filtered through celite, and concentrated to afford of 4-(5-fluoro-2-methoxy-phenyl)-4-hydroxypiperidine (0.95 g 69% yield) as a yellow oil.

1. customthe system purged with N2 for 5 min
2. additionTo the solution, 1.95 g of 10% palladium on carbon was added
3. customThe system was again purged with N2 for 5 minutes
4. additionfollowed by addition of 2 mL formic acid (88%)
5. additionAt this point, a further 2 mL of formic acid (88%) was added
6. waitThe reaction was continued for 2.5 days
7. filtrationThe mixture was filtered through celite
8. concentrationconcentrated