反应详情

4-Chloro-N-(2-oxo-azepan-3-yl)-benzenesulfonamide (0.45 g, 1.50 mmol), 1-bromomethyl-4-difluoromethyl-benzene (0.66 g, 3.00 mmol), potassium carbonate (2.09 g, 15.0 mmol) and potassium iodide (0.05 g, 0.20 mmol) in 15 ml dimethylformamide were stirred at 65° C. for 5 hours. Extraction with water/ethylacetate and chromatography on silicagel with ethylacetate/heptane (90/10 to 1/0) yielded 0.63 g (94%) 4-chloro-N-(4-difluoromethyl-benzyl)-N-(2-oxo-azepan-3-yl)-benzenesulfonamide as white solid, MS: m/e (%)=443.0 (MH+, 100).

1. extractionExtraction with water/ethylacetate and chromatography on silicagel with ethylacetate/heptane (90/10 to 1/0)