Synthesis and x‐ray crystal structures of isonipecotinamide derivatives as reverse amide analogues of fentanyl

Abstract

AbstractSeveral isonipecotinamide derivatives which represent reverse amide derivatives of the potent analgetic agent fentanyl were prepared and evaluated for analgetic activity. The synthetic approaches utilized and stereochemical assignments are discussed. The most potent compound, 3, displayed much weaker analgetic activity than fentanyl itself.