反应详情

温度

130 °C

To a solution of {1-[2-bromo-4-(3-fluoro-pyridine-4-ylcarbamoyl)-phenyl]-ethyl}-carbamic acid tert-butyl ester (1094 μmol) and 3-aminophenylboronic acid (2 eq) in a mixture of DME/ethanol/1N Na2CO3: 1/1/1 (10 ml) was added Pd tetrakis (0.05 eq). The reaction mixture was heated in the microwave at 130° C. for 1.5 hours. The reaction mixture was cooled to RT and diluted with water and citric acid and extracted with EtOAc. The combined organic layers were washed with water and brine. The organic layer was dried over MgSO4 and the solvent was removed under reduced pressure. The compound was purified by column chromatography (silicagel, DCM/MeOH gradient).

1. temperatureThe reaction mixture was cooled to RT
2. extractionextracted with EtOAc
3. washThe combined organic layers were washed with water and brine
4. dry with materialThe organic layer was dried over MgSO4
5. customthe solvent was removed under reduced pressure
6. customThe compound was purified by column chromatography (silicagel, DCM/MeOH gradient)