反应详情

To 3-amino-2,6-difluoro-benzoic acid benzyl ester (3, 6.00 g, 22.8 mmol) in 150 mL of dichloromethane, pyridine (2.76 mL, 34.2 mmol) and propane-1-sulfonyl chloride (4, 3.80 mL, 33.8 mmol) were added. The reaction was stirred at room temperature overnight, then poured into water, and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered and the filtrate concentrated under vacuum. The desired compound was isolated with silica gel column chromatography to give a colorless oil (5, 7.0 g, 83.1%). MS(ESI) [M+H+]+=370.1.

1. extractionextracted with ethyl acetate
2. washThe organic layer was washed with brine
3. dry with materialdried over anhydrous sodium sulfate
4. filtrationfiltered
5. concentrationthe filtrate concentrated under vacuum