반응 #40981

반응 방정식

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

2-bromo-6-fluoropyridine

Na2CO3

PPh3

→

title compound

수율 57.6%

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

수율 57.6%

용매

n-PrOH

반응 조건

후처리

1. 1
   온도at reflux for 3 hours
2. 2
   기타The solvent was evaporated under vacuum
3. 3
   기타the crude was partitioned between water and ethyl acetate
4. 4
   건조The organic phase was dried (Na2SO4)
5. 5
   기타evaporated
6. 6
   기타The crude was triturated with iPrOH

실험 절차

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).

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