反应详情

温度

80 °C

To a solution of 1-(5-allyl-4-chloro-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-2,2,2-trifluoro-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]ethanol (250 mg, 0.5 mmol) in 3 mL of dioxane was added 2 mL of water followed by 2 mL of trifluoroacetic acid. The mixture was warmed at 80° C. for 1.5 hours, cooled to room temperature and made basic with saturated sodium bicarbonate, diluted with water, and extracted with EtOAc. The combined organic layers were dried, filtered, and evaporated. The residue was purified by flash chromatography eluting with MeOH—CH2Cl2 (0-2% gradient) to provide 129 mg (53%) of the title compound as a white solid. MS m/z 484.33 (MH+).

1. temperaturecooled to room temperature
2. extractionextracted with EtOAc
3. customThe combined organic layers were dried
4. filtrationfiltered
5. customevaporated
6. customThe residue was purified by flash chromatography
7. washeluting with MeOH—CH2Cl2 (0-2% gradient)