反应详情

To a solution of pyridine-3-sulfonyl chloride (70 mg, 0.40 mmol) in THF (4 mL) were added 3,5-dichloro-N-(3-chloro-5-((isobutylamino)methyl)benzyl)-2-hydroxy-N-isobutylbenzenesulfonamide (100 mg, 0.20 mmol) and Et3N (0.14 mL, 0.98 mmol). The reaction mixture was stirred at rt for 3 h. The mixture was concentrated. To the residue was added 1 N NaOH/THF/MeOH. After 4 h, the mixture was concentrated and the residue was purified by preparative HPLC. Fractions containing the desired product were combined, concentrated, and lyophilized to give the desired product as a white solid (60 mg, 40%).

1. concentrationThe mixture was concentrated
2. additionTo the residue was added 1 N NaOH/THF/MeOH
3. waitAfter 4 h
4. concentrationthe mixture was concentrated
5. customthe residue was purified by preparative HPLC
6. additionFractions containing the desired product
7. concentrationconcentrated