Abstract
The optical isomers of 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran hydrochloride (1a, b) (befunolol·HCl) were synthesized by using (S)-1, 2-O-isopropylideneglycerol (4) as a common chiral building block, and their β-adrenergic blocking activities were examined. The (S)-(-)-isomer 1b was about 300 times more potent than the (R)-(+)-isomer 1a on an atrial preparation.
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