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, 50.0 mg, 0.144 mmol), KF (42.6 mg, 0.719 mmol) and 1-methylperazine-2-one hydrochloride (67.0 mg, 0.431 mmol) were suspended in NMP (0.4 mL). The RM was stirred at 180° C. for 4 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 3.75 min (conditions 5), (tR 11.35 min (conditions 2), MH+=425.9, 1H-NMR in DMSO-d6: 8.07 (s, 1H); 7.80 (d, 1H); 7.52 (s, 1H); 7.36 (d, 1H); 7.05 (d, 1H); 4.85 (m, 1H); 4.01 (d, 1H); 3.95 (s, 3H); 3.78 (d, 1H); 3.62 (m, 2H); 3.27 (m, 2H); 2.81 (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