Nitrogen-bridged conformationally constrained etorphine analogues. Synthesis and biological evaluation

Article abstract of DOI:10.1021/jm00394a016

Three N-C8-bridged analogues 4-6 of the opiate etorphine (3) were synthesized and evaluated for opiate agonism and antagonism. In each case ring closure was effected by intramolecular N-alkylation with a suitably developed C8 side chain. Another key synth