反应详情

温度

90 °C

(rac)-2,2,2-Trifluoro-N-(6-{hydroxy-[6-(1-methyl-1H-pyrazol-4-yl)-imidazo[1,2-b]pyridazin-3-yl]-methyl}-imidazo[1,2-a]pyridin-2-yl)-acetamide (Example 153, 120 mg, 0.263 mmol) was dissolved in THF/MeOH 1:1 (2 mL). K2CO3 was added (363 mg, 2.63 mmol) with water (1 mL) and the RM was heated over night at 90° C. After concentration under reduced pressure, the residue was purified by flash chromatography (CombiFlash® Companion System®, with 12 g RediSep® silica gel column, DCM/MeOH=8:2->DCM/MeOH/H2O/ammonia=80:19:0.5: 0.5) to afford the title compound (MH+=361, 1H NMR in DMSO-d6: .8.5 (s, 1H); 8.4 (s, 1H); 8.1 (s, 1H); 8.0 (d, 1H); 7.6 (s, 1H); 7.5 (d, 1H), 7.1 (q, 2H), 7.0 (s, 1H); 6.2 (s, 2H); 5.0 (s, 2H); 3.9 (s, 3H)).

1. concentrationAfter concentration under reduced pressure
2. customthe residue was purified by flash chromatography (CombiFlash® Companion System®, with 12 g RediSep® silica gel column, DCM/MeOH=8:2->DCM/MeOH/H2O/ammonia=80:19:0.5: 0.5)