反应详情

温度

140 °C

To a solution of Example 57 (50 mg, 0.151 mmol) in THF (4 mL) was added 2-fluoro-6-pyridinecarboxylic acid (53 mg, 0.378 mmol) and sodium tert-butoxide (73 mg, 0.755 mmol). The mixture was heated to 140° C. under microwave irradiation for 90 minutes, cooled to r.t. and concentrated in vacuo. The residue was purified by preparative HPLC (Method 6) to give the title compound (15 mg, 22%) as an off-white solid. δH (CDCl3) 8.07 (1H, d, J 2.4 Hz), 7.94-7.91 (2H, m), 7.24-7.16 (1H, m), 7.00 (1H, d, J 8.9 Hz), 6.85 (1H, dd, J 8.9 and 2.6 Hz), 5.45 (1H, s), 4.52-4.20 (2H, m), 4.20-4.01 (2H, m), 2.84 (2H, s), 1.38 (6H, s). LCMS (ES+) 453.0 (M+H)+, RT 2.94 minutes (Method 1).

1. temperaturecooled to r.t.
2. concentrationconcentrated in vacuo
3. customThe residue was purified by preparative HPLC (Method 6)