反应详情

温度

100 °C

To a 100 mL RBF, was added 5-(3-bromo-phenyl)-2-[2-(isopropylamino-methyl)-pyrrolidin-1-yl]-3-methyl-6-pyridin-4-yl-3H-pyrimidin-4-one (0.4 g, 0.82 mmol), 30 mL toluene, and cyclopropyl boronic cid (86 mg, 1.0 mmol). The mixture was degassed by nitrogen bubbled through for 1 h. After added Pd(PPh)4 (30 mg, 0.025 mmol) and NaOtBu (0.24 g, 2.5 mmol), the mixture was warmed up to 100° C. and stirred for 1 h under nitrogen. The mixture was cooled down to rt, and vacuumed down all volatile composites. After purified by flash chromatography, the title compound was obtained in 0.1 g as pale yellow solid. MS (ES+): 444 (M+H)+; (ES−): 4442 (M−H).

1. customThe mixture was degassed by nitrogen
2. custombubbled through for 1 h
3. temperatureThe mixture was cooled down to rt
4. customAfter purified by flash chromatography