Reaktion #40981

Reaktionsgleichung

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

2-bromo-6-fluoropyridine

Na2CO3

PPh3

→

title compound

Ausbeute 57.6%

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

Ausbeute 57.6%

Lösungsmittel

n-PrOH

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturat reflux for 3 hours
2. 2
   SonstigeThe solvent was evaporated under vacuum
3. 3
   Sonstigethe crude was partitioned between water and ethyl acetate
4. 4
   TrocknenThe organic phase was dried (Na2SO4)
5. 5
   Sonstigeevaporated
6. 6
   SonstigeThe crude was triturated with iPrOH

Vorschrift

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).

Quelle