反应详情

温度

60 °C

Propane-1-sulfonyl chloride (0.0871 mL, 0.774 mmol) was dissolved in 10% Na2CO3 (1.65 mL, 1.55 mmol) at room temperature. 5-Amino-2-fluorobenzoic acid (0.100 g, 0.645 mmol) was added and heated to 60° C. overnight. Propane-1-sulfonyl chloride (0.0871 mL, 0.774 mmol) was added again, and the reaction mixture was heated at 60° C. for another hour. The reaction mixture was cooled to room temperature, diluted with water, taken to a pH of 10 with 10% Na2CO3 and extracted with DCM (2×). The reaction mixture was then taken to a pH of 2 with 1N HCl, extracted with DCM (3×) and concentrated to a solid, 2-fluoro-5-(propylsulfonamido)benzoic acid (29%).

1. temperaturethe reaction mixture was heated at 60° C. for another hour
2. temperatureThe reaction mixture was cooled to room temperature
3. extractionextracted with DCM (2×)
4. extractionextracted with DCM (3×)
5. concentrationconcentrated to a solid, 2-fluoro-5-(propylsulfonamido)benzoic acid (29%)