反应详情

To a mixture of 5-(pyrazin-2-yl)picolinic acid 41-4 (28 mg, 0.14 mmol), 4-(aminomethyl)-1-(2-(trifluoromethyl)pyridin-4-yl)pyridin-2(1H)-one 56-7 (35 mg, 0.13 mmol) and O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluroniumhexafluorophosphate (HATU) (49 mg, 0.13 mmol) in DMF (1.0 mL) was added DIEA (0.09 mL, 0.52 mmol) at room temperature. The mixture was stirred at room temperature for 2 hours. The reaction mixture was diluted into DMSO and purified by HPLC to give N-((2-oxo-1-(2-(trifluoromethyl)pyridin-4-yl)-1,2-dihydropyridin-4-yl)methyl)-5-(pyrazin-2-yl)picolinamide 56 as a white solid. MS m/z 453.2 (M+1). 1H NMR 400 MHz (DMSO-d6) δ 9.57 (t, 1H), 9.40 (d, 1H), 9.36 (dd, 1H), 8.86 (d, 1H), 8.77 (dd, 1H), 8.69 (m, 2H), 8.16 (dd, 1H), 8.07 (d, 1H), 7.84 (dd, 1H), 7.73 (d, 1H), 6.37 (dd, 1H), 6.31 (b, 1H), 4.36 (d, 2H).

1. custompurified by HPLC