反应详情

温度

100 °C

A reaction vessel was charged with 2-bromo-6-cyclopropylpyrazine (1.27 g, 6.39 mmol, Combi-Phos Catalysts Inc.) and Pd(PPh3)4 (308 mg, 0.27 mmol). The tube was sealed. A solution of 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazole (1.30 g, 5.33 mmol) in dioxane (18 mL) and 2 M Na2CO3 (aq.) (8.0 mL, 16.0 mmol) were added. The reaction was stirred and heated at 100° C. overnight. After cooling to RT, the organic layer was separated and dried over anhydrous Na2SO4, filtered and concentrated. The crude was purified by silica gel chromatography, eluting with a gradient of 0-50% EtOAc in hexanes, to provide 5-(6-cyclopropylpyrazin-2-yl)-1H-indazole (575 m g, 2.43 mmol, 46% yield) as an off-white solid. MS (ESI, pos. ion) m/z: 237.2 (M+1).

1. customThe tube was sealed
2. temperatureAfter cooling to RT
3. customthe organic layer was separated
4. dry with materialdried over anhydrous Na2SO4
5. filtrationfiltered
6. concentrationconcentrated
7. customThe crude was purified by silica gel chromatography
8. washeluting with a gradient of 0-50% EtOAc in hexanes