反应详情

5-Iodo-1-{3-[(1S,5R)-1-(4-trifluoromethyl-phenyl)-3-aza-bicyclo[3.1.0]hex-3-yl]-propyl}-1H-pyrimidine-2,4-dione (Prep40, 150 mg, 0.3 mmol) was dissolved in degassed MeOH (4 mL). 2-Methoxy-pyridine-3-boronic acid (136 mg, 0.9 mmol), KF (155 mg, 2.7 mmol), and Pd(OAc)2 (15 mg, 10% weight) were added and the mixture was heated to vigorous reflux for 2.5 hours. The mixture was diluted with MeOH, loaded on SCX cartridge washing with MeOH and MeOH/NH3 95:5. The solvent was evaporated under vacuum and the residue was purified by flash chromatography with ethyl acetate to give the title compound as free base (70 mg, 48% yield).

1. temperaturethe mixture was heated
2. temperatureto vigorous reflux for 2.5 hours
3. washwashing with MeOH and MeOH/NH3 95:5
4. customThe solvent was evaporated under vacuum
5. customthe residue was purified by flash chromatography with ethyl acetate