反应详情

A mixture of 2,4-dichloro-5-chloromethyl-pyrimidine (3.70 g, 18.7 mmol) (from Example 1b supra), 2-fluoro-4-methoxy-phenylamine (2.40 g, 17.0 mmol) (from Example 14a supra) and potassium carbonate (4.70 g, 34.0 mmol) in acetone (100 mL) was stirred at room temperature for 18 hours. The precipitate was filtered off and the solution was concentrated under reduced pressure. The residue was diluted with ethyl acetate and washed with water and brine, dried over magnesium sulfate, filtered and concentrated under reduced pressure. This residue was purified by flash chromatography eluting with ethyl acetate-hexanes (1:4) to give [(2,4-dichloropyrimidin-5-yl)methyl]-(4-methoxyphenyl)-amine. (Yield 3.99 g, 78%).

1. filtrationThe precipitate was filtered off
2. concentrationthe solution was concentrated under reduced pressure
3. additionThe residue was diluted with ethyl acetate
4. washwashed with water and brine
5. dry with materialdried over magnesium sulfate
6. filtrationfiltered
7. concentrationconcentrated under reduced pressure
8. customThis residue was purified by flash chromatography
9. washeluting with ethyl acetate-hexanes (1:4)