反应详情

Heat a mixture of dimethyl-pyrrolidin-3-(S)-yl-amine (3.0 g, 26.3 mmoL), 5-bromo-2-fluoro-pyridine (4.62 g, 26.3 mmol), potassium carbonate (7.98 g, 57.8 mmol) in acetonitrile (91 mL) at 80° C. overnight. Allow the mixture to cool to RT, filter with CH2Cl2, and concentrate. Purify the crude material by flash chromatograph, eluting with 5% MeOH (2N NH3)/CH2Cl2 to give 3.55 g (50%) of the title compound. LC-MS/ES m/z (81Br) 272.3 [M+H]+.

1. temperatureHeat
2. filtrationfilter with CH2Cl2
3. concentrationconcentrate
4. customPurify the crude material by flash chromatograph
5. washeluting with 5% MeOH (2N NH3)/CH2Cl2