反应详情

温度

70 °C

To a stirred solution of 1,1-dimethylethyl [2-(3-(4-{[(dimethylamino)carbonyl]amino}phenyl)-4-{2-[3-(hydroxymethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl}-1H-pyrazol-1-yl)ethyl]methylcarbamate (1.24 g, 2.0 mMol) in CHCl3 (100 mL) was added activated MnO2 (2.5 g, 28.7 mMol). The reaction was stirred and refluxed (70° C. oil bath) for 8 h, cooled to RT, filtered through a pad of Celite®, rinsed with CHCl3, and evaporated to dryness under vacuum. Purification by flash chromatography on silica gel (5 to 10% MeOH in (1:1) EtOAc/CHCl3) provided the title compound (0.94 g, 77%) as a pale yellow solid. ESMS [M+H]+: 608.6.

1. temperaturecooled to RT
2. filtrationfiltered through a pad of Celite®
3. washrinsed with CHCl3
4. customevaporated to dryness under vacuum
5. customPurification by flash chromatography on silica gel (5 to 10% MeOH in (1:1) EtOAc/CHCl3)