A new family of beta-blocking drugs is described. The originality of the new molecules lies in their functionalized hydrophobic folded structure, the basic part of which contains a benzocyclobutene ring. Excellent beta 2-blocker selectivity has been obtained with some of these compounds. Interestingly, this selectivity was not modified toward beta 1-blocker activity by introduction of the usual beta 1 inducer groups.

Durch Cycloaddition der den Verbindungen (I) entsprechenden Arine mit den Enolaten (II) erhält man die Schlüsselverbindungen (III) und (IV), die über die Phenole (V) in die Phenolether (VI) umgewandelt werden.