Synthesis of Procaterol Derivative Having a Piperidylmethanol Group and Its β-Adrenoceptor Stimulant Activities

A procaterol derivative (6) having a piperidylmethanol group was synthesized by the nucleophilic reaction of a 5-formylcarbostyril derivative with pyridyllithium, followed by selective catalytic reductions to afford the erythro-isomer. Compound 6 showed non-selective β-adrenoceptor agonist activities like those of l-isoproterenol in an in vivo assay using anesthetized dogs.