Synthesis of 5-(3-tert-Butylamino-2-hydroxypropoxy)-8-hydroxy-3, 4-dihydrocarbostyril Hydrochloride and Its β-Adrenergic Blocking Activity

Abstract
5-(3-tert-Butylamino-2-hydroxypropoxy)-8-hydroxy-3,4-dihydrocarbostyril hydrochloride, the main metabolite of the new adrenergic .beta.-blocking agent, 5-(3-tert-butylamino-2-hydroxypropoxy)-3,4-dihydrocarbostyril hydrochloride (Carteolol hydrochloride), was synthesized, and its antagonism against the positive chronotropic and hypotensive actions of isoproterenol was examined in anesthetized dogs. This compound was a little more active than Carteolol hydrochloride.