反应详情

温度

180 °C

6-Chloro-3-[(S)-1-(4,6-difluoro-1-methyl-1H-indazol-5-yl)-ethyl]-imidazo[1,2-b]pyridazine (Intermediate Q, 36.6 mg, 0.105 mmol), KF (30.6 mg, 0.526 mmol) and 1-acetylpiperazine (40.5 mg, 0.316 mmol) were suspended in NMP (0.4 mL). The RM was stirred at 180° C. for 3.5 h. The mixture was diluted with EtOAc and washed with NaHCO3 10% (2×) and water (4×). The combined organic layers were dried over Na2SO4, filtered and concentrated. The residue was purified by flash chromatography and afforded the title compound as a light brown foam (tR 3.80 min (conditions 5), tR 13.31 min (conditions 3), MH+=440.3, 1H-NMR in DMSO-d6: 8.12 (s, 1H); 7.79 (d, 1H); 7.52 (s, 1H); 7.39 (d, 1H); 7.04 (d, 1H); 4.84 (m, 1H); 3.96 (s, 3H); 3.36 (m, 8H); 1.99 (s, 3H); 1.79 (d, 3H)).

1. washwashed with NaHCO3 10% (2×) and water (4×)
2. dry with materialThe combined organic layers were dried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified by flash chromatography