Beta:adrenergic-blocking, amino-hydroxy-propoxy isoquinoline derivs. - prepd. by reacting epoxy-propoxy-(2)-acyl-isoquinolines with amines

摘要

New 2-acyl-isoquinoline derivs. are cpds. of formula (I) and salts: (where R1 is H or CH3; R2 is H or lower alkyl; R3 is H or OCHof and R4 is isopropyl or tert-butyl). (I) have high adrenergic beta-receptor blocking activity coupled with low toxicity. The beta-blocking activity can be detected on cardiac, vascular and bronchial receptors. Some cpds. (I) have a particular effect on the beta-receptors of the heart and are suitable for treating functional heart disorders. In general, (I) can be used for treating functional heart disorders, such as tachycardia, tachycardic disorders of heart rhythm, extrsystoles, angina pectoris, hyperkinetic heart syndrome etc., as well as hypertension. Specific cpds. (I) include 2-acetyl-1,2,3,4-tetrahydro-6-(2-hydroxy-3-tert-butylaminopropoxy- )-isoquinoline. In an example, this is prepd. by refluxing 2-acetyl-6-(2,3-epoxypropoxy)-1,2,3,4-tetrahydroisoquinoline withtert-butylamine.