反应详情

To a solution of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl chloride (1.688 mmol, 450 mg) in acetonitrile (24.8 mL) was added 2-amino-4-fluoropyridine (4.22 mmol, 473 mg). The reaction mixture was stirred at room temperature for 1.5 h. The reaction mixture was concentrated to a small volume, 3% aq. citric acid solution (18 mL) was added and the mixture was extracted with dichloromethane (2×15 mL). The combined organic layer was washed with 3% aq. citric acid solution, dried over magnesium sulfate, filtered and evaporated to afford 542.2 mg of N-(4-fluoropyridin-2-yl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide (94%) as an off-white solid.

1. concentrationThe reaction mixture was concentrated to a small volume, 3% aq. citric acid solution (18 mL)
2. additionwas added
3. extractionthe mixture was extracted with dichloromethane (2×15 mL)
4. washThe combined organic layer was washed with 3% aq. citric acid solution
5. dry with materialdried over magnesium sulfate
6. filtrationfiltered
7. customevaporated