ChemInform Abstract: Synthesis and Biological Evaluation of Dibenz[b,f][1,5]oxazocine Derivatives for Agonist Activity at ϰ‐Opioid Receptor.

Abstract

Synthesis and Biological Evaluation of Dibenz[b,f][1,5]oxazocine Derivatives forAgonist Activity at κ-Opioid Receptor. -A short synthetic route to title compounds (II) is developed using an optimized Pd-catalyzed intramolecular cycloamination reaction as the key step. Receptor-binding assay using dynorphin-125 I demonstrates that derivative (IIc) shows selective κ-opioidergic property. The aryl amine basicity seems to be important for the cycloamination and no cyclization product is obtained from nitro--substituted aryl amine (Ie). -(MITRA, S.; BANERJEE, T. S.; HOTA, S. K.; BHATTACHARYA, D.; DAS, S.; CHATTOPADHYAY*, P.; Eur. J. Med. Chem. 46 (2011) 5, 1713-1720, http://dx.