β Adrenergic blocking agents. Nitrogen heteroaryl substituted 2 propanolamines and ethanolamines

Article abstract of DOI:10.1021/jm00268a010

A series of some 20 novel 2 propanolamines of type I was prepared by reaction of Het CH₂Li with the properly substituted aminoacetonitrile, followed by hydrolysis and reduction. The most potent β adrenergic blocking activity was found in the phenanthridine, quinoline, and isoquinoline series, the phenanthridine being almost 10 times as active as propranolol. Some ethanolamine homologs of the phenanthridine and quinoline series were prepared for comparison, the former being toxic, the latter somewhat more active than the corresponding 2 propanolamine.