反应详情

温度

0 °C

A 1 M solution (0.18 ml) of a borane/tetrahydrofuran complex was added dropwise at 0° C. into a solution of 1-[1-(4-fluorophenethyl)piperidin-4-yl]-6-methoxyindole (24 mg) in trifluoroacetic acid (1 ml) over 2 min followed by stirring at 0° C. for 30 min. Af ter the completion of the reaction, water (0.1 ml) was added thereto and the resulting reaction solution was concentrated under reduced pressure. The resulting residue was dissolved in a 2 N aqueous solution of sodium hydroxide and stirred at room temperature for 10 min. The mixture was extracted with methylene chloride. The organic layer was separated and dried over magnesium sulfate. After concentrating the solvent under reduced pressure, the resulting residue was purified by preparative TLC to give 1-[1-(4-fluorophenethyl)piperidin-4-yl)]-6-methoxyindoline (10 mg) (yield: 35%).

1. additionwas added
2. customthe resulting reaction solution
3. concentrationwas concentrated under reduced pressure
4. dissolutionThe resulting residue was dissolved in a 2 N aqueous solution of sodium hydroxide
5. stirringstirred at room temperature for 10 min
6. extractionThe mixture was extracted with methylene chloride
7. customThe organic layer was separated
8. dry with materialdried over magnesium sulfate
9. concentrationAfter concentrating the solvent under reduced pressure
10. customthe resulting residue was purified by preparative TLC