反应详情

温度

100 °C

To a solution of 120 mg of 1-(t-butoxycarbonyl)-4-(6-bromo-imidazo[1,2-a]pyridin-3-yl)-piperidine and 78 mg of phenylboronic acid in 5 mL of toluene and 2.5 mL of ethanol was added 8 mg of tetrakis(triphenylphosphine)-palladium(0), followed by 0.85 mL of 1.25N sodium hydroxide solution. The reaction was stirred at 100° C. for 8 hours. The mixture was concentrated under reduced pressure and the mixture was partitioned between EtOAc and water. Aqueous layer was extracted with EtOAc (3×). The combined organic phase was washed with brine and dried over MgSO4. The residue was purified by flash chromatography with 50% EtOAc in hexanes followed by 100% EtOAc to give 141 mg of the title compound as a viscous oil, which was used in next step without further purification.

1. concentrationThe mixture was concentrated under reduced pressure
2. customthe mixture was partitioned between EtOAc and water
3. extractionAqueous layer was extracted with EtOAc (3×)
4. washThe combined organic phase was washed with brine
5. dry with materialdried over MgSO4
6. customThe residue was purified by flash chromatography with 50% EtOAc in hexanes