反应详情

HATU (0.086 g, 0.227 mmol) was added to a solution of 3-{[3-(aminomethyl)-6-chloro-2-fluorophenyl]oxy}-5-chlorobenzonitrile (0.047 g, 0.151 mmol), 6-(acetylamino)-1H-indole-2-carboxylic acid (0.033 g, 0.151 mmol) and DIPEA (0.040 mL, 0.227 mmol) in DMF (1 mL). The mixture was stirred at RT for 2 h. The reaction mixture was diluted with ethyl acetate and water. The organic layer was washed with water and dried over sodium sulfate, and the solvent was evaporated. The resulting oil was triturated with methylene chloride:methanol. The resulting solid was collected by filtration and dried under vacuum to give the title compound (0.024 g, 31%) as an off-white solid. 1H NMR (400 MHz, DMSO-d6): δ ppm 11.46 (s, 1H), 9.85 (s, 1H), 9.01 (m, 1H), 7.91 (s, 1H), 7.80 (s, 1H), 7.40-7.53 (m, 4H), 7.35 (t, 1H), 7.11 (m, 2H), 4.51 (d, 2H), 2.00 (s, 3H). MS: m/z 511 (M+1).

1. washThe organic layer was washed with water
2. dry with materialdried over sodium sulfate
3. customthe solvent was evaporated
4. customThe resulting oil was triturated with methylene chloride
5. filtrationThe resulting solid was collected by filtration
6. customdried under vacuum