反应详情

In a 1 dram vial, 3-{[3-(aminomethyl)-6-chloro-2-fluorophenyl]oxy}-5-chlorobenzonitrile (25 mg, 0.080 mmol), DIPEA (0.014 mL, 0.080 mmol) and 5-isoxazolecarboxylic acid (9.09 mg, 0.080 mmol) were dissolved in DMF (1 mL). HATU was added (30.6 mg, 0.080 mmol) and the solution stirred overnight. The reaction mixture was diluted to 2 mL with MeOH. Purification was accomplished by Reverse-Phase HPLC (water/acetonitrile with 0.1% TFA) to afford the title compound (0.015 g, 46%) as a white solid. 1H NMR (400 MHz, Acetone-d6): δ ppm 8.65 (br. s., 1H), 8.57 (d, 1H), 7.63 (t, 1H), 7.46-7.53 (m, 1H), 7.41-7.46 (m, 1H), 7.35-7.41 (m, 2H), 6.99 (d, 1H), 4.69 (d, 2H). LCMS m/z 405.9 (M+1).

1. customPurification