反应详情

温度

120 °C

To a solution of 5-bromo-3-(1-isopropyl-1H-[1,2,3]triazol-4-yl)-pyridin-2-ylamine (300 mg, 1.06 mmol) and (3-methoxy-4-(methoxycarbonyl)phenyl)boronic acid (245 mg, 1.16 mmol) in 1,4-dioxane (10.0 mL)/water (5.0 mL) was added Cs2CO3 (1.0 g, 3.18 mmol) at room temperature. The reaction mixture was degassed with argon for 30 min. Then Pd(PPh3)4 (61 mg, 0.05 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 aqueous layer was neutralized with 1N HCl, extracted with DCM (2×50 mL), washed with brine solution (20 mL), dried over anhydrous Na2SO4 and solvent was evaporated under reduced pressure. The crude compound was washed with diethyl ether to afford 260 mg (yield: 69.33%) 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. extractionextracted with DCM (2×50 mL)
5. washwashed with brine solution (20 mL)
6. dry with materialdried over anhydrous Na2SO4 and solvent
7. customwas evaporated under reduced pressure
8. washThe crude compound was washed with diethyl ether