168164-00-9

Upstream product

• 168163-96-0 4,4-difluoro-1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-one 
• 168163-92-6 4,4-difluoro-1-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-5H-1-benzoazepin-5-one 
• 168163-93-7 4-fluoro-1-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-5H-1-benzoazepin-5-one 
• 168163-95-9 4,4-difluoro-1,2,3,4-tetrahydro-benzo[b]azepin-5-one 
• 24310-36-9 1-tosyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one 
• 5927-18-4 trimethyl phosphonoacetate 
• 168163-97-1 1-(4-aminobenzoyl)-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-one 

Downstream Products

• 168162-46-7 (E)-methyl {4,4-difluoro-1-[4-(2-phenylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-ylidene}acetate 
• 168162-52-5 (E)-{4,4-difluoro-1-[4-(2-phenylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-ylidene}acetic acid 

Relevant academic research and scientific papers

Highly potent and orally active non-peptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 4'-[(4,4,-difluoro-5-methylidene-2,3,4,5-tetrahydro-1H-1-benzoazepin-1-yl)car bonyl]-2-phenylbenzanilide derivatives

A series of compounds structurally related to 4'-[(4,4-difluoro-5-methylidene-2,3,4,5-tetrahydro-1H-1-benzoazepin-1-yl)carb onyl]-2-phenylbenzanilide were synthesized and evaluated for arginine vasopressin (AVP) antagonistic activity. Compounds with a (Z)-olefin geometry at the 5-position of benzoazepine possessed potent affinity for both the V(1A) and V2 receptors. Further study has shown that one of these derivatives, (Z)-4'-({4,4-difluoro-5-[(4-dimethylaminopiperidino)carbonylmethylene]-2,3,4 ,5-tetrahydro-1H-1-benzoazepin-1-yl}carbonyl)-2-phenylbenzanilide monohydrochloride (29, YM-35471), exhibits exceptionally potent affinity for both of V(1A) and V2 receptors, even when administered orally. The synthesis and pharmacological properties of this compound are detailed in this paper.