Synthesis and β-Adrenergic Blocking Activity of 2-(N-Substituted amino)-1, 2, 3, 4-tetrahydronaphthalen-1-ol Derivatives

Abstract

In a search for a new structural type of β-adrenergic antagonist. a series of trans-2-(N-substituted amino)-1, 2, 3, 4-tetrahydronaphthalen-1-ol derivatives (3-36) was synthesized in several steps from 3, 4-dihydro-1 (2H)-naphthalenone (37) having a variety of substituents at the 5-, 6-, 7-and 8-positions. Compounds 3-36 were tested in vitro for β-adrenergic activity. Among them, 2-benzhydrylamino-6-chloro-1, 2, 3, 4-tetrahydronaphthalen-1-ol (28c) was found to show a fairly potent β-adrenergic blocking activity.