反应详情

温度

80 °C

N-(2-Chloro-5-{4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-[(4-methylphenyl)sulfonyl]-1H-indazol-6-yl}-3-pyridinyl)methanesulfonamide (50 mg, 0.084 mmol) and morpholine (0.015 ml, 0.169 mmol) were placed in acetonitrile (5 ml) and the mixture heated at 80° C. for 4 h. Further morpholine (15 μl) was added and the reaction was continued to heat overnight. The mixture was cooled to room temperature and the mixture loaded onto an SCX (5 g) cartridge. The cartridge was washed with methanol and then eluted with 2M ammonia in methanol. The mixture was purified by chromatography on silica (20 g) cartridge eluting with 0-100% ethyl acetate in cyclohexane followed by 0-20% methanol to give the title compound (52 mg).

1. temperatureto heat overnight
2. temperatureThe mixture was cooled to room temperature
3. washThe cartridge was washed with methanol
4. washeluted with 2M ammonia in methanol
5. customThe mixture was purified by chromatography on silica (20 g) cartridge
6. washeluting with 0-100% ethyl acetate in cyclohexane