反应详情

温度

95 °C

A mixture of 6-methoxy-4-iodopyridin-3-amine (9.5 g, 38 mmol), 5-bromo-2-fluoropyridin-3-ylboronic acid (16.7 g, 76 mmol), and 1,1′-[bis(diphenylphosphino)ferrocene]dichloropalladium(II) (1.5 g, 2 mmol) in 1N aqueous potassium fluoride (95 mL) and acetonitrile (200 mL) was heated at 95° C. for 16 h. The cooled reaction mixture was diluted with water (100 mL) and extracted with DCM (3×100 mL). The combined organic layer was dried over sodium sulfate, filtered, and evaporated to afford a residue which was purified by flash chromotagraphy (silica, 120 g column, ISCO, 0-40% ethyl acetate in hexanes) to afford the title compound as a yellow/orange solid (8.0 g, 71%).

1. customThe cooled reaction mixture
2. extractionextracted with DCM (3×100 mL)
3. dry with materialThe combined organic layer was dried over sodium sulfate
4. filtrationfiltered
5. customevaporated
6. customto afford a residue which
7. customwas purified by flash chromotagraphy (silica, 120 g column, ISCO, 0-40% ethyl acetate in hexanes)