反应详情

A mixture of 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole (70 mg, 0.300 mmol) and 5-fluoroindane-2-carbaldehyde (49 mg, 0.300 mmol) in CH3OH (4 mL) and acetic acid (0.2 mL) was stirred at rt for 15 minutes. NaCNBH3 (40 mg, 0.635 mmol) was added and then the reaction mixture was stirred for 1 hour. The solvent was removed and the residue was diluted with CH2Cl2. The organic layers were washed with saturated NaHCO3, brine, and dried over Na2SO4. The organic extracts were removed under the reduced pressure and the residue was purified by flash chromatography (5% CH3OH in CH2Cl2) to afford 6-fluoro-1-[1-(5-fluoro-indan-2-ylmethyl)-piperidin-4-yl]-5-methyl-1H-benzoimidazole (28 mg, 24%) as a white solid.

1. stirringthe reaction mixture was stirred for 1 hour
2. customThe solvent was removed
3. additionthe residue was diluted with CH2Cl2
4. washThe organic layers were washed with saturated NaHCO3, brine
5. dry with materialdried over Na2SO4
6. customThe organic extracts were removed under the reduced pressure
7. customthe residue was purified by flash chromatography (5% CH3OH in CH2Cl2)