反应详情

To a solution of tert-butyl (1-(4-(5-(2,6-difluorophenyl)-1-tosyl-1H-indol-3-yl)-6-methoxypyrimidin-2-yl)piperidin-4-yl)carbamate (60 mg, 0.087 mmol) in dioxane (0.8 mL) was added 7M aq.NaOH (1 mL) and the mixture was heated at 90° C. for 6 h. The reaction was quenched with water and the suspension was filtered. The resulting solid was washed with water and dried. The crude was purified with basic alumina chromatography to give tert-butyl (1-(4-(5-(2,6-difluorophenyl)-1H-indol-3-yl)-6-methoxypyrimidin-2-yl)piperidin-4-yl)carbamate (25 mg, 54%). 1H-NMR (300 MHz, DMSO-d6): δ 11.80 (brs, 1H), 8.58 (s, 1H), 8.26 (s, 1H), 7.40-7.55 (m, 2H), 7.18-7.26 (m, 4H), 6.85 (d, J=7.5 Hz, 1H) 6.49 (s, 1H), 4.66 (d, J=11.7 Hz, 2H), 3.84 (s, 3H), 3.52 (brs, 2H), 2.97-3.05 (m, 2H), 1.7 (brs, 2H), 1.38 (s, 9H).

1. customThe reaction was quenched with water
2. filtrationthe suspension was filtered
3. washThe resulting solid was washed with water
4. customdried
5. customThe crude was purified with basic alumina chromatography