反应详情

A suspension of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (5.29 g, 27.3 mmol), 2-bromo-N-methylpropanamide (9.05 g, 54.5 mmol) and potassium carbonate (5.65 g, 40.9 mmol) in 136 ml acetone was refluxed for 68 hours. The white suspension was filtered through Celite with acetone washes; and the filtrate was concentrated and purified via silica gel chromatography (80 mm; 1 L 65% ethyl acetate/hexanes to 80% ethyl acetate/hexanes) to afford the title compound.

1. temperaturewas refluxed for 68 hours
2. filtrationThe white suspension was filtered through Celite with acetone washes
3. concentrationand the filtrate was concentrated
4. custompurified via silica gel chromatography (80 mm; 1 L 65% ethyl acetate/hexanes to 80% ethyl acetate/hexanes)