反应详情

温度

81 °C

In a flask, combine 5-bromomethyl-2-fluoro-4-iodo-pyridine (6.13 g, 19.4 mmol), morpholine (3.38 g, 38.8 mmol) and dry CH3CN (100 mL) under nitrogen. Add N,N-diisopropylethylamine (6.76 mL, 38.80 mmol, 2 M THF solution). Heat at 81° C. for 2 h and cool to RT. Dilute with DCM and wash with water and aqueous saturated sodium chloride. Separate the organic layer from the aqueous layer and dry over magnesium sulfate. After filtration, concentrate in vacuo to give the title compound 6.23 g (100%). MS (ES) m/z 323 [M+1]+.

1. customIn a flask, combine
2. temperaturecool to RT
3. washwash with water and aqueous saturated sodium chloride
4. customSeparate the organic layer from the aqueous layer
5. dry with materialdry over magnesium sulfate
6. filtrationAfter filtration
7. concentrationconcentrate in vacuo