Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetami d e derivatives as novel arginine vasopressin V sub(2 receptor agonists)

The present work describes the discovery of novel series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetam i de derivatives as arginine vasopressin (AVP) V sub(2 receptor agonists. By replacing the amide juncture in YM-35278 with a direct ring connection gave compound 10a, which acts as a V) sub(2) receptor agonist. These studies provided the potent, orally active non-peptidic V sub(2 receptor agonists 10a and 10j.)