反应详情

温度

180 °C

6-Chloro-3-[(S)-1-(6-fluoro-1-methyl-1H-indazol-5-yl)-ethyl]-imidazo[1,2-b]pyridazine (Intermediate E, 50.0 mg, 0.152 mmol), KF (26.4 mg, 0.455 mmol) and 1-methylperazine-2-one hydrochloride (51.9 mg, 0.455 mmol) were suspended in NMP (1 mL). The RM was stirred at 180° C. for 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 3.66 min (conditions 5), (tR 12.22 min (conditions 2), MH+=408.2, 1H-NMR in DMSO-d6: 7.92 (s, 1H); 7.83 (d, 1H); 7.49 (m, 3H); 7.11 (d, 1H); 4.78 (m, 1H); 4.00 (d, 1H); 3.95 (s, 3H); 3.86 (d, 1H); 3.67 (m, 2H); 3.30 (m, 2H); 2.80 (s, 3H); 1.71 (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