反应详情

A mixture of 1-(4-fluorophenyl)-5-nitro-2-oxo-1,2-dihydropyridine-3-carboxylic acid (40 mg, 0.14 mmol) and 4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorobenzenamine (35 mg, 0.14 mmol, Compound B of Example 132) in DMF (1 mL) was stirred with BOP reagent (100 mg, 0.23 mmol) and triethylamine (0.1 mL) at 50° C. for 1 h. The reaction mixture was cooled to room temperature and diluted with water. The solid that formed was collected, washed with aqueous sodium bicarbonate solution, 1 N HCl solution, and water to afford the title compound (54 mg, 76%). 1H NMR (DMSO-d6) δ 12.19 (s, 1H), 11.04 (s, 1H), 9.37 (d, 1H, J=2.6 Hz), 9.03 (d, 1H, J=2.6 Hz), 8.18 (d, 1H, J=5.5 Hz), 8.01 (dd, 1H, J=10.2, 2.6 Hz), 7.71 (m, 2H), 7.61 (m, 1H), 7.46 (m, 4H), 6.55 (d, 1H, J=5.5 Hz), 6.36 (s, 1 Hz); MS(ESI+) m/z 504 (M+H)+.

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