反应详情

To a solution of N-(2-aminophenyl)-4-chlorobenzenesulfonamide (0.5 mmol, prepared as in Example 11) in DCM (1 mL) and pyridine (1 mL), benzofuran-2-sulfonyl chloride (0.55 mmol), prepared as above, was added at RT and the reaction mixture was then allowed to stir at RT overnight or until the reaction was complete as determined by TLC or LC-MS. The reaction mixture was then diluted with DCM (5 mL). The organic phase was washed with 10% aqueous HCl (5 mL), water (5 mL) and brine (5 mL). The organic phase was dried over anhydrous sodium sulfate, and concentrated under vacuum. The residue obtained was purified by flash column chromatography eluting with DCM/EtOAc to afford 92 mg benzofuran-2-sulfonic acid [2-(4-chlorobenzenesulfonylamino)phenyl]-amide. LC: Tr 1.13 min, MS: 464.0 (M+1)+.

1. additionwas added at RT
2. washThe organic phase was washed with 10% aqueous HCl (5 mL), water (5 mL) and brine (5 mL)
3. dry with materialThe organic phase was dried over anhydrous sodium sulfate
4. concentrationconcentrated under vacuum
5. customThe residue obtained
6. customwas purified by flash column chromatography
7. washeluting with DCM/EtOAc