ISOCARBOSTYRIL DERIVATIVE

摘要

NEW MATERIAL:A compound of formulaI(R is branched alkyl of 4-4 carbon atoms) and its acid adduct. EXAMPLE:4-(3-tert.-Butylamino-2-hydroxy)propoxyisocarbostyril hydrochloride. USE:A remedy for cardiopathies such as hypertension, angina pectoris or arrhythmia: its has stronger and long-lasting activity of beta-adrenergic blocking. PREPARATION:The reaction of 4-hydroxyisocarbostyril of formula II with an epihalogenohydrin of formula III (X is halogen) is carried out in the presence of a base at 35-70 deg.C for 1-7hr to give a compound of formula IV (Y is hydroxyl; Z is halogen or Y and Z may link to each other to form an epoxy ring). The product reacts with an amine of RNH2 to give the compound of formulaI.