Conformationally defined adrenergic agents. 1. Design and synthesis of novel. alpha. 2-selective adrenergic agents: electrostatic repulsion based conformational …
A previous report of the adrenergic selectivity of 2-and 6-fluoronorepinephrine prompted us to formulate a hypothesis that accounted for this selectivity on the basis of a conformational preference induced by electrostatic repulsion between the aromatic fluorine atom and the side-chain hydroxyl group. A series of nitrogen-substituted catechol (aminomethyl) benzocyclobutenes, indanes, tetralins, and benzocycloheptenes were prepared, and ...
