反应详情

A mixture of 4-chloro-5-methyl-2-methylsulfanyl-pyrimidine (1.24 g, 7.1 mmol), pyridine-3-boroni acid (1.04 g, 8.46 mmol), Na2CO3 (863 mg, 7.76 mmol), PPh3 (186 mg, 0.71 mmol) and Pd(OAc)2 (40 mg) in n-PrOH (50 ml) was refluxed for 2 hours. The solvent was then evaporated under vacuum and the crude was partitioned between water and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-1) to afford 1.28 g of the title compound as a white solid (83% yield)

1. temperaturewas refluxed for 2 hours
2. customThe solvent was then evaporated under vacuum
3. customthe crude was partitioned between water and ethyl acetate
4. dry with materialThe organic phase was dried (Na2SO4)
5. customevaporated
6. customThe crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-1)