反应详情

温度

-5 °C

A suspension of 2,4-dichloro-6-(methylsulfonylmethyl)pyrimidine (10.56 g) in DCM (230 mL) was stirred magnetically (under nitrogen) and cooled to −5° C. Triethylamine (6.78 mL) was added followed by the dropwise addition of a solution of morpholine (3.85 mL) in DCM (30 mL) maintaining the reaction temperature below −5° C. The reaction was stirred at room temperature for 1 hour and then the organic mixture washed with water (300 mL). The organic phase was dried (MgSO4), filtered and evaporated to a brown solid which was chromatographed on silica, eluting with 50% ethyl acetate in DCM, to give the desired material (6.81 g) as a white solid.

1. temperaturemaintaining the reaction temperature below −5° C
2. stirringThe reaction was stirred at room temperature for 1 hour
3. washthe organic mixture washed with water (300 mL)
4. dry with materialThe organic phase was dried (MgSO4)
5. filtrationfiltered
6. customevaporated to a brown solid which
7. customwas chromatographed on silica
8. washeluting with 50% ethyl acetate in DCM