Hydroxy-3-tert. butylamino-propoxy-acetamido-phenyl oxadiazole - beta-adrenolytic suitable for treating angina pectoris, hypertonia and arrhythmia

摘要

butylaminopropoxy) -5-acetamidophenyl) -1,3,4-oxadiazole of formula (I) and its physioogically acceptable acid addn. salts are new. (I) has a specific beta adrenolytic and blood pressure lowering effect and can therefore be used to treat angina pectoris, hypertonia and arrhythmia. (I) can be used orally or parenterally. Suitable daily doses are 50-100 mg, pref pref. divided into smaller doses throughout the day. (I) has a very long half-life. In an example (I) was prepd. by heating 3g 2(2-hydroxy-5- acetamidophenyl)-1,3,4-oxadiazole in 30 ml epibromohydrin with 2 drops of piperidine for 12 hrs. at 50 deg.C. After sepg. unreacted starting material, the bromohydrin was distd. off and the residue rubbed with diisopropyl ether. 0.5g 2-(2-(2,3-epoxypropoxy) -5-acetamidophenyl) -1,3,4-oxadiazole of m.pt. 173-175 deg.C were obtd. 0.4 g of this cpd. were stirred for 15 hrs. at 20-25 deg in 30 ml MeOH and 30 ml tert butylamine. The soln. was concd. by evapn. and the residue recrystd. from toluene. 0.5g of (I) of m.pt. 157-160 deg.C were obtd.