反应详情

To a solution of 2-fluoro-5-(trifluoromethyl)benzonitrile (8.0 g, 42.3 mmol, Aldrich) in tetrahydrofuran (50 mL) were added sodium hydride (1.9 g, 46.5 mmol) and (S)-(1-methylpyrrolidin-2-yl)methanol (5.5 mL, 46.5 mmol, Aldrich). After stirring at room temperature for 3 hours, the reaction mixture was quenched with saturated NaHCO3 (30 mL). The aqueous layer was extracted with ethyl acetate (3×30 mL). The combined organic layers were washed with brine (50 mL), dried Na2SO4, filtered and concentrated under reduced pressure to afford 12.0 g (100%) of the title compound. LCMS (APCI+) m/z 285 (M+H)+.

1. customthe reaction mixture was quenched with saturated NaHCO3 (30 mL)
2. extractionThe aqueous layer was extracted with ethyl acetate (3×30 mL)
3. washThe combined organic layers were washed with brine (50 mL), dried Na2SO4
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure