反应详情

温度

100 °C

To a solution of (R)-1-(2-aminopyrimidin-4-yl)ethanol (6a) (250 mg) in dry N-methylmorpholine (4 mL) at ambient temperature was added potassium 2-methylpropan-2-olate (222 mg) and the solution was left to stir for 30 min then 2-fluoro-3-(trifluoromethyl)pyridine (282 mg) was added the mixture was stirred for 10 min at ambient temperature and then heated to 100° C. with microwave irradiation for 2 minutes then cooled and quenched into water (50 mL). The precipitated solid was filtered and washed with water and air dried under a slight vacuum. The semi-dried material was taken up in methylene chloride and dried over magnesium sulfate to which activated charcoal was added then filtered through a bed of dicalite and evaporated to give the title compound (359 mg), MS (ES): m/z 285 [M+H]+.

1. waitthe solution was left
2. stirringwas stirred for 10 min at ambient temperature
3. temperaturethen cooled
4. customquenched into water (50 mL)
5. filtrationThe precipitated solid was filtered
6. washwashed with water and air
7. customdried under a slight vacuum
8. dry with materialdried over magnesium sulfate to which activated charcoal
9. additionwas added
10. filtrationthen filtered through a bed of dicalite
11. customevaporated