反应详情

温度

120 °C

To a solution of (3-fluoro-4-(morpholine-4-carbonyl)phenyl)boronic acid (269 mg, 1.06 mmol) and of 5-bromo-3-(1-isopropyl-1H-[1,2,3]triazol-4-yl)-pyridin-2-ylamine (250 mg, 0.886 mmol) in 1,4-dioxane (10.0 mL)/water (5.0 mL) was added Cs2CO3 (863 mg, 2.65 mmol) at room temperature. The reaction mixture was degassed with argon for 30 min. Then Pd(PPh3)4 (51 mg, 0.04 mmol) was added and allowed to stir at 120° C. for 30 min in CEM micro wave. The reaction mixture was cooled to RT, diluted with EtOAc (50 mL) and washed with water (50 mL). The organic layer was washed with brine solution (20 mL), dried over anhydrous Na2SO4 and solvent was evaporated under reduced pressure to afford crude compound. Crude compound was purified by column using 100-200 mesh silica gel. The column was eluted with 5% MeOH in DCM to afford 125 mg (yield: 34.43%) of the title compound as pale yellow solid.

1. customThe reaction mixture was degassed with argon for 30 min
2. temperatureThe reaction mixture was cooled to RT
3. washwashed with water (50 mL)
4. washThe organic layer was washed with brine solution (20 mL)
5. dry with materialdried over anhydrous Na2SO4 and solvent
6. customwas evaporated under reduced pressure
7. customto afford crude compound
8. customCrude compound was purified by column
9. washThe column was eluted with 5% MeOH in DCM