Reacción #40981

Ecuación de reacción

2,4-Dimethoxy-pyrimidine-5-boronic acid

2-bromo-6-fluoropyridine

Na2CO3

PPh3

→

title compound

Rendimiento 57.6%

5-(6-Fluoro-pyridin-2-yl)-2,4-dimethoxy-pyrimidine

Rendimiento 57.6%

Disolventes

n-PrOH

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturaat reflux for 3 hours
2. 2
   OtroThe solvent was evaporated under vacuum
3. 3
   Otrothe crude was partitioned between water and ethyl acetate
4. 4
   SecadoThe organic phase was dried (Na2SO4)
5. 5
   Otroevaporated
6. 6
   OtroThe crude was triturated with iPrOH

Procedimiento

2,4-Dimethoxy-pyrimidine-5-boronic acid (966 mg, 5.3 mmol) was dissolved in degassed n-PrOH (60 ml) and then 2-bromo-6-fluoropyridine (850 mg, 4.8 mmol), Na2CO3 (1.676 g, 15.8 mmol), PPh3 (400 mg, 1.52 mmol) and Pd(OAc)2 (116 mg) were added. The suspension was stirred at reflux for 3 hours. The solvent was evaporated under vacuum and the crude was partitioned between water and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated. The crude was triturated with iPrOH to give 650 mg of the title compound as a white powder (52% yield).

Fuente