反应详情

To a mixture of 1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxylic acid (45 mg, 0.19 mmol), HOBt (20 mg) and EDCI.HCl (80 mg, 0.31 mmol) in DMF (2.5 mL) was added 4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorobenzenamine (56 mg, 0.18 mmol) at rt, and the reaction mixture was stirred over the weekend at rt. It was directly purified by preparative HPLC to afford the product (35 mg, 30%) as a beige-colored TFA salt solid. 1H NMR (CD3OD) δ 12.21 (s, 1H), 8.60 (dd, 2H, J=9.9, 1.6 Hz), 8.01 (d, 1H, J=12.6 Hz), 7.90 (dd, 1H, J=7.6, 1.6 Hz), 7.74 (s, 1H), 7.45-7.37 (m, 5H), 7.24 (t, 2H, J=8.2 Hz), 6.89 (d, 1H, J=6.6 Hz), 6.65 (t, 1H, J=6.6 Hz), 4.03 (s, 3H), 4.00 (s, 3H); MS(ESI+) m/z 530.2 (M+H)+.

1. customIt was directly purified by preparative HPLC