反应详情

温度

125 °C

A mixture of chloride 6-chloro-2-(3-fluorophenethylamino)-N-(pyridin-3-ylmethyl)nicotinamide (100 mg, 0.260 mmol), trans-1-propen-1-yl boronic acid (27 mg, 0.312 mmol), PdCl2(dppf)2 (14 mg, 0.026 mmol), 2N K2CO3(0.39 mL, 0.78 mmol) and THF (1.5 mL) was stirred at 125° C. for 30 min. The mixture was filtered through the silica gel pad and washed with EtOAc. The filtrate was concentrated to dryness and purified on RP-HPLC using a mixture of acetonitrile and H2O to give (E)-2-(3-fluorophenethylamino)-6-(prop-1-enyl)-N-(pyridin-3-ylmethyl)nicotinamide as a pale yellow solid (59 mg, 86%). LRMS (M+H+) m/z 391.2.

1. filtrationThe mixture was filtered through the silica gel pad
2. washwashed with EtOAc
3. concentrationThe filtrate was concentrated to dryness
4. custompurified on RP-HPLC
5. additiona mixture of acetonitrile and H2O