反应详情

温度

85 °C

(S)-(1-(7-(3,4-Difluorophenyl)-3-iodo-2-methylpyrazolo[1,5-a]pyrimidin-5-yl)pyrrolidin-2-yl)methanol (62 mg), 4-methoxyphenylboronic acid (27 mg) and tetrakis(triphenylphosphine)palladium (10 mg) are added to toluene (8 mL), ethanol (3 mL) and 1 N NaHCO3 aqueous solution (1.5 mL) and stirred for 6 hours under argon atmosphere at 85° C. After cooling to room temperature, the reaction solvent is removed by distillation under reduced pressure. The remainder is extracted with ethyl acetate and water. The organic layer is washed with brine and dehydrated with anhydrous MgSO4. The dehydrated organic layer is distilled under reduced pressure, concentrated and purified by column chromatography to yield the target compound (58 mg).

1. temperatureAfter cooling to room temperature
2. customthe reaction solvent is removed by distillation under reduced pressure
3. extractionThe remainder is extracted with ethyl acetate and water
4. washThe organic layer is washed with brine
5. distillationThe dehydrated organic layer is distilled under reduced pressure
6. concentrationconcentrated
7. custompurified by column chromatography