反应详情

温度

80 °C

A mixture of 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (237 mg, 1.139 mmol), 3-((2-chloropyridin-4-yl)oxy)-2,4-dimethyl-6-nitropyridine (245 mg, 0.876 mmol), K2CO3 (363 mg, 2.63 mmol) and Pd(PPh3)4 (51 mg, 0.044 mmol) in dioxane (4 mL) and water (1 mL) was sparged with Ar, heated at 80° C. for 24 h, then cooled to RT. The mixture was diluted with EtOAc. Washed with satd. NaHCO3, then brine, dried over Na2SO4 and concentrated to dryness to afford 2,4-dimethyl-3-((2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl)oxy)-6-nitropyridine (100% yield assumed) which was used without further purification. MS (ESI) m/z: 326.1 (M+H+).

1. customwas sparged with Ar
2. temperaturecooled to RT
3. additionThe mixture was diluted with EtOAc
4. washWashed with satd
5. dry with materialNaHCO3, then brine, dried over Na2SO4
6. concentrationconcentrated to dryness