SULFONAMIDE DERIVATIVE

摘要

1381184 Sulphonamides BOEHRINGER INGELHEIM GmbH 30 March 1972 [1 April 1971] 15156/72 Heading C2C [Also in Division C4] Novel compounds (I) (including salts thereof). where R 1 is H or alkyl, R 2 is alkyl or NR, R 2 signifies pyrrolidino or piperidino, R 3 is H or OH, R 4 is H, Me or Et and R 5 is H, alkyl optionally substituted by a heterocyclic group, or an aralkyl or aryloxyalkyl group wherein the aryl portion may be substituted, are obtained by standard methods. The following compounds are also prepared: 4 - benzyloxy - 3 - dimethylamino - sulphonamidoacetophenone, 4 - benzyloxy - 3 - dimethylaminosulphonamide - # - bromoacetato - phenone, 1 - (4 - benzyloxy - 3 - dimethylamino - sulphonamidophenyl) - # - 1 - phenoxyisopropyl - aminoacetophenone, 1 - (4 - benzyloxy - 3 - dimethylaminosulphonamidophenyl) - 1 - hydroxy - 2 - (1- phenoxyisopropylamino)ethane, 4 - benzyloxy - 3 dimethylaminosulphonamido - # - N - benzyl - N- ethyl - amino - acetophenone, 4 - hydroxy - 3- dimethylaminosulphonamido - # - ethylaminoacetophenone hydrochloride, 4 - benzyloxy - 3- methylaminosulphonamido - # - bromoacetophenone , 4 - benzyloxy - 3 - pyrrolidinosulphonamido - # - bromoacetophenone, 4 - benzyloxy - 3 - dimethylaininosulphonamido - # - azidoacetophenone, 4 - hydroxy - 3 - dimethyl - aminosulphonamido - # - aminoacetophenone hydrobromide, 4 - benzyloxy - 3 - dimethylaminosulphonamido - α - dibenzylaminopropiophenone, 1 - (4 - benzyloxy - 3 - dimethylamino - sulphonamidophenyl) - 1 - hydroxy - 2 - dibenzylaminopropane and 4 - hydroxy - 3 - dimethylaminosulphonamidobenzyl cyanide. Pharmaceutical preparations showing broncholytic effect and useful in the treatment of hypertension contain (I) as active ingredient. Administration may be orally, parenterally and enterally.