反应详情

温度

80 °C

To a pressure vessel was added cesium carbonate (0.61 g, 1.9 mmol), PdCl2(dppf)-CH2Cl2 adduct (26 mg, 0.031 mmol), 1-(6-chloro-3-fluoropyridin-2-yl)-2,2-difluoro-2-(quinolin-6-yl)ethanone oxime (0.26 g, 0.63 mmol) and 3,5-difluorophenylboronic acid (0.15 g, 0.94 mmol) in anhydrous DMF (5 mL) and water (1 mL). The mixture flushed with argon, sealed and stirred at 80° C. for one hour. The suspension was concentrated, triturated with water and filtered to afford a tan solid, purification by MPLC (eluted with a gradient of 20 to 50% ethyl acetate in hexanes) afforded the product as a white solid (23 mg, 9%). MS m/z=410.0 [M+1]+ Calc'd for C22H11F4N3O: 409.3.

1. customThe mixture flushed with argon
2. customsealed
3. concentrationThe suspension was concentrated
4. customtriturated with water
5. filtrationfiltered
6. customto afford
7. customa tan solid, purification by MPLC (
8. washeluted with a gradient of 20 to 50% ethyl acetate in hexanes)