反应详情

温度

120 °C

A mixture of 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 (Prep 40, 150 mg, 0.3 mmol), 2-fluoro-5-chloropyridine-3-boronic acid (142 mg, 0.9 mmol), KF (157 mg, 2.7 mmol), and Pd(OAc)2 (20 mg) in degassed MeOH (4 ml) was placed in a microwave oven and warmed at 120° C. for 25 minutes. The mixture was filtered, MeOH was evaporated and the crude partitioned between brine and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated; the crude was purified by flash chromatography with ethyl acetate-NH4OH (0.5%) to give the title compound (10 mg, 6% yield).

1. customwas placed in a microwave oven
2. filtrationThe mixture was filtered
3. customMeOH was evaporated
4. customthe crude partitioned between brine and ethyl acetate
5. dry with materialThe organic phase was dried (Na2SO4)
6. customevaporated
7. customthe crude was purified by flash chromatography with ethyl acetate-NH4OH (0.5%)