反应详情

温度

125 °C

A mixture of 6-chloro-2-(3-fluorophenethylamino)-N-(pyridin-3-ylmethyl)nicotinamide (1.0 g, 2.6 mmol), 2-cyanophenyl boronic acid (460 mg, 3.12 mmol), PdCl2(dppf)2 (140 mg, 0.26 mmol), K2CO3 (1.08 g, 7.8 mmol) and anhydrous DMF (8 mL) was degassed with nitrogen for 10 min. The mixture was then stirred at 125° C. for 1 hr. The mixture was filtered through the silica gel pad and washed with EtOAc. The filtrate was concentrated to dryness and purified by silica gel flash chromatography to give the desired product 6-(2-cyanophenyl)-2-(3-fluorophenethylamino)-N-(pyridin-3-ylmethyl)nicotinamide as a pale yellow solid (740 mg, 63%). LRMS (M+H+) m/z 452.1.

1. customwas degassed with nitrogen for 10 min
2. filtrationThe mixture was filtered through the silica gel pad
3. washwashed with EtOAc
4. concentrationThe filtrate was concentrated to dryness
5. custompurified by silica gel flash chromatography