反应详情

3-[(3,5-dimethoxyphenyl)methylamino]-N-methyl-propanamide (Intermediate 98; 1 g, 3.96 mmol) was dissolved in DCM (10 mL) and triethylamine (0.68 mL, 4.36 mmol). 5-bromo-2,4-dichloropyrimidine (Aldrich; 993 mg, 4.36 mmol) was added and the mixture stirred at room temperature for 18 hours. The mixture was diluted with DCM and washed with water, brine, dried (MgSO4), filtered and evaporated to give a yellow gum which was purified on a 40 g ISCO companion eluting with 50-70% ethyl acetate in iso-hexane to give the title compound as a white solid (461 mg, 26%).

1. washwashed with water, brine
2. dry with materialdried (MgSO4)
3. filtrationfiltered
4. customevaporated
5. customto give a yellow gum which
6. customwas purified on a 40 g ISCO companion
7. washeluting with 50-70% ethyl acetate in iso-hexane