反应详情

2,4-Dimethoxy-pyrimidine-5-boronic acid (1.33 g, 7.27 mmol) was dissolved in degassed n-PrOH (20 ml) and then 2-iodo-pyrazine (1.0 g, 4.85 mmol), Na2CO3 (1.02 g, 9.70 mmol), PPh3 (127 mg, 0.48 mmol) and Pd(OAc)2 (54 mg) were added. The suspension was stirred at reflux for 4 hours. The solvent was evaporated under vacuum and the crude was partitioned between water and DCM. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by flash chromatography eluting with DCM-MeOH—NH4OH (99-1-0.1) to give 481 mg of the title compound (45% yield).

1. temperatureat reflux for 4 hours
2. customThe solvent was evaporated under vacuum
3. customthe crude was partitioned between water and DCM
4. dry with materialThe organic phase was dried (Na2SO4)
5. customevaporated
6. customThe crude was purified by flash chromatography
7. washeluting with DCM-MeOH—NH4OH (99-1-0.1)