反应详情

2,4-Dimethoxy-pyrimidine-5-boronic acid (1 g, 5.46 mmol) was dissolved in degassed n-PrOH (30 ml) and then 2-cyano-3-bromopyridine (950 mg, 5.19 mmol), Na2CO3 (1.65 g, 15.56 mmol), PPh3 (393 mg, 1.5 mmol) and Pd(OAc)2 (114 mg, 0.51 mmol) were added. The suspension was stirred at reflux for 3 hours. After cooling, the solvent was evaporated under vacuum and the crude was partitioned between water and ethyl acetate. The organic phase washed with brine, dried (Na2SO4) and evaporated. The residue was triturated with iPrOH to give 1 g of the title compound as a white powder (76% yield).

1. temperatureat reflux for 3 hours
2. temperatureAfter cooling
3. customthe solvent was evaporated under vacuum
4. customthe crude was partitioned between water and ethyl acetate
5. washThe organic phase washed with brine
6. dry with materialdried (Na2SO4)
7. customevaporated
8. customThe residue was triturated with iPrOH