Synthesis of constrained L-phenylalanine derivatives incorporating a benzazepinone or an azepinone ring as VCAM/VLA-4 antagonists

Article abstract of DOI:10.1016/S0040-4039(01)01926-8

Novel constrained L-phenylalanine derivatives incorporating a benzazepinone or an azepinone ring were synthesized in 13 and 8 steps, respectively, employing a key base-catalyzed intramolecular cyclization reaction. The product, 2, was comparable in potenc