反应详情

温度

-5 °C

2,4-Dichloro-6-(methylsulfonylmethyl)pyrimidine (30 g, 0.13 mol) was dissolved in dichloromethane and stirred (under nitrogen) at −5° C. Triethylamine (17.4 mL, 0.13 mol) was added to give a clear brown solution. (3S)-3-Methylmorpholine was dissolved in dichloromethane and added dropwise keeping the reaction below −5° C. The cooling bath was then removed and the mixture stirred for 1 hour. The reaction mixture was heated at reflux for 2 hours, then the reaction mixture was washed with water, dried then evaporated. The crude material was purified by preparative HPLC to give the desired material as a solid (19.3 g).

1. customto give a clear brown solution
2. additionadded dropwise
3. customthe reaction below −5° C
4. customThe cooling bath was then removed
5. stirringthe mixture stirred for 1 hour
6. temperatureThe reaction mixture was heated
7. temperatureat reflux for 2 hours
8. washthe reaction mixture was washed with water
9. customdried
10. customthen evaporated
11. customThe crude material was purified by preparative HPLC