반응 #41014

반응 방정식

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

2-fluoro-6-methyl-3-iodopyridine

Na2CO3

PPh3

→

title compound

수율 75.5%

5-(2-Fluoro-6-methyl-pyridin-3-yl)-2,4-dimethoxy-pyrimidine

수율 75.5%

용매

n-PrOH

반응 조건

후처리

1. 1
   온도at reflux for 2.5 hours
2. 2
   기타The solvent was evaporated under vacuum
3. 3
   기타the crude was partitioned between water and DCM
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 (1.16 g, 6.32 mmol) was dissolved in degassed n-PrOH (22 ml) and then 2-fluoro-6-methyl-3-iodopyridine (870 mg, 3.67 mmol), Na2CO3 (778 mg, 7.34 mmol), PPh3 (96 mg, 0.37 mmol) and Pd(OAc)2 (41 mg added in three portions) were added. The suspension was stirred at reflux for 2.5 hours. The solvent was evaporated under vacuum and the crude was partitioned between water and DCM. The organic phase was dried (Na2SO4) and evaporated. The crude was triturated with iPrOH to give 691 mg of the title compound (75% yield).

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