反应详情

The 4-(4-aminopiperidin-1-yl)-benzoic acid ethyl ester (15.7 g, 63.2 mmol) obtained in Example 7(1) was dissolved in THF (200 ml), and a 2M sodium carbonate aqueous solution (63 ml) was added thereto. Subsequently, benzyloxycarbonyl chloride (11.7 ml, 82.2 mmol) was added thereto, followed by stirring at room temperature for 2 hours. Water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with water and saturated sodium chloride, and then dried over anhydrous sodium sulfate. After the desiccant was filtered off, the solid obtained by evaporation under reduced pressure was collected by filtration and dried under reduced pressure, thereby obtaining 4-(4-benzyloxycarbonylaminopiperidin-1-yl)-benzoic acid ethyl ester (18.0 g, 74%) as a white solid.

1. extractionfollowed by extraction with ethyl acetate
2. washThe organic layer was washed with water and saturated sodium chloride
3. dry with materialdried over anhydrous sodium sulfate
4. filtrationAfter the desiccant was filtered off
5. customthe solid obtained by evaporation under reduced pressure
6. filtrationwas collected by filtration
7. customdried under reduced pressure