反应详情

tert-Butyl ((1-((3-(2-(cyclopropylamino)-2-oxoethoxy)phenyl)sulfonyl)-5-(2-fluorophenyl)-1H-pyrrol-3-yl)methyl)(methyl)carbamate 3a (122 mg, 0.22 mmol) was dissolved in 8 mL of dichloromethane. The reaction solution was cooled in an ice bath, and 2 mL of trifluoroacetic acid were dropwise added. After removing the ice bath, the reaction solution was stirred at room temperature for 2 h. 20 mL of saturated sodium bicarbonate solution were added, and the reaction solution was extracted with dichloromethane (20 mL×3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography with elution system A to obtain the title product N-cyclopropyl-2-(3-((2-(2-fluorophenyl)-4-((methylamino)methyl)-1H-pyrrol-1-yl)sulfonyl)phenoxy)acetamide 3 (80 mg, a colorless oil) in 80% yield.

1. temperatureThe reaction solution was cooled in an ice bath
2. customAfter removing the ice bath
3. addition20 mL of saturated sodium bicarbonate solution were added
4. extractionthe reaction solution was extracted with dichloromethane (20 mL×3)
5. dry with materialdried over anhydrous sodium sulfate
6. filtrationfiltered
7. concentrationthe filtrate was concentrated under reduced pressure
8. customThe resulting residue was purified by silica gel column chromatography with elution system