Synthesis and biological evaluation of dibenz(b,f)(1,5)oxazocine derivatives for agonist activity at kappa-opioid receptor.

摘要

A short and high yield synthetic route to dibenz[b,f][1,5]oxazocines has been developed using Pd catalyzed intramolecular cycloamination reaction. Receptor binding assay using [125I]-dynorphin demonstrated that one of the derivative, 5b showed selective kappa-opioidergic property.