反应详情

温度

0 °C

2-(4-((4-(4-Aminobenzyl)piperidin-1-yl)methyl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol (0.336 mmol, 150 mg) and 2-phenylacetyl chloride (0.504 mmol, 0.067 mL, 78 mg) were combined in dichloromethane (3 mL) and cooled to 0° C. Triethylamine (0.672 mmol, 0.093 mL, 68.0 mg) was added and the mixture allowed to stir at 0° C. for 2 hours before allowing to warm to room temperature and stirring overnight. The reaction was diluted with dichloromethane and washed with water. The mixture was filtered through a hydrophobic frit and concentrated under vacuum. The residue was purified by flash chromatography on silica gel (eluent: dichloromethane-10% methanol/dichloromethane gradient) to afford the title compound (124.4 mg).

1. temperatureto warm to room temperature
2. stirringstirring overnight
3. washwashed with water
4. filtrationThe mixture was filtered through a hydrophobic frit
5. concentrationconcentrated under vacuum
6. customThe residue was purified by flash chromatography on silica gel (eluent: dichloromethane-10% methanol/dichloromethane gradient)