反应 #40961

反应方程式

5-Iodo-2,4-dimethoxy-pyrimidine

2-methylphenyl boronic acid

Na2CO3

PPh3

→

title compound

收率 46.3%

2,4-Dimethoxy-5-o-tolyl-pyrimidine

收率 46.3%

溶剂

n-PrOH

反应条件

后处理

1. 1
   温度at reflux for 3 hours
2. 2
   其他The solvent was evaporated
3. 3
   其他the crude was partitioned between water and DCM
4. 4
   干燥The organic phase was dried (Na2SO4)
5. 5
   其他evaporated
6. 6
   其他The crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-9)

实验过程

5-Iodo-2,4-dimethoxy-pyrimidine (1 g, 3.75 mmol) was dissolved in degassed n-PrOH (25 mL) and then 2-methylphenyl boronic acid (766 mg, 3.8 mmol), Na2CO3 (865 mg, 8.16 mmol), PPh3 (215 mg, 0.8 mmol) and Pd(OAc)2 (50 mg, 5.67 mmol) were added. The suspension was stirred at reflux for 3 hours. The solvent was evaporated and the crude was partitioned between water and DCM. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by flash chromatography with ethyl acetate-petroleum ether (1-9) to give 400 mg of the title compound (46% yield).

来源