反应详情

To a solution of 4-fluoro-3-nitrobenzenesulfonamide (1.26 g) and 1-cyclopropylpiperidin-4-amine (0.802 g) in tetrahydrofuran (20 mL) was added N,N-diisopropylethylamine (2.22 g) and 4-dimethylaminopyridine (35 mg). The mixture was heated at reflux for 18 hours and upon cooling was diluted with ethyl acetate (200 mL) and aqueous NaHCO3. The crude product was isolated by concentration of the organic layer and was purified on silica gel, which was eluted with 5% methanolic ammonia in methylene chloride to give the title compound.

1. temperatureThe mixture was heated
2. temperatureat reflux for 18 hours
3. temperatureupon cooling
4. customThe crude product was isolated by concentration of the organic layer
5. customwas purified on silica gel, which
6. washwas eluted with 5% methanolic ammonia in methylene chloride