反应详情

2,4-Di-tert-butoxy-pyrimidine-5-boronic acid (500 mg, 1.75 mmol) was dissolved in n-PrOH (5 mL) and then 2-bromo-3-methylthiophene (236 μl, 2.1 mmol), Na2CO3 (556 mg, 5.25 mmol), PPh3 (133 mg, 0.52 mmol) and Pd(OAc)2 (40 mg, 0.17 mmol) were added. The suspension was stirred at reflux for 2.5 hours. The solvent was evaporated and the crude was dissolved in water and extracted with Et2O. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-99) to give 170 mg of the title compound as a white solid (32% yield).

1. temperatureat reflux for 2.5 hours
2. customThe solvent was evaporated
3. dissolutionthe crude was dissolved in water
4. extractionextracted with Et2O
5. dry with materialThe organic phase was dried (Na2SO4)
6. customevaporated
7. customThe crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-99)