Abstract Sulfochlorination of 2?螫?xo??2, 3, 4, 5??tetrahydro??1 H??benzo [b] azepine led to regioselective formation of the corresponding 7??chlorosulfonyl derivative. Starting from this reagent, a large number of substituted 2??oxo??7??sulfamoyl??2, 3, 4, 5??tetrahydro??1 H??benzo [b] azepines were obtained. This approach is amenable to combinatorial production of the title compounds, which possess promising therapeutic potential.