168163-99-3

Upstream product

• 5927-18-4 trimethyl phosphonoacetate 
• 168163-97-1 1-(4-aminobenzoyl)-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-one 
• 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 
• 122-04-3 4-nitro-benzoyl chloride 
• 183171-54-2 methyl (2Z)-(4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetate 
• 183171-60-0 methyl (Z)-[4,4-difluoro-1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene]acetate 

Downstream Products

• 168162-45-6 (Z)-methyl {4,4-difluoro-1-[4-(2-phenylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-ylidene}acetate 
• 168162-80-9 methyl (Z)[1-[4-(2-chlorobenzoyl)amino]benzoyl-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene]acetate 
• 168162-75-2 methyl (Z)-[4,4-difluoro-1-[4-(2-methylbenzoyl)amino]benzoyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene]acetate 
• 168162-78-5 methyl (Z)-[4,4-difluoro-1-[4-(2-isopropoxybenzoyl)amino]benzoyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene]acetate 
• 168162-76-3 methyl (Z)-[4,4-difluoro-1-[4-(2methoxybenzoyl)amino]benzoyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene]acetate 
• 168162-95-6 methyl (Z)-[1-[4-(2,6-dimethoxybenzoyl)amino]benzoyl-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzazepin-5ylidene]acetate 
• 881309-37-1 methyl (Z)-{4,4-difluoro-1-[4-(5-methyloxazole-4-carbonylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene}acetate 
• 881309-36-0 methyl (Z)-{4,4-difluoro-1-[4-(2-methylfuran-3-carbonylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene}acetate 
• 168162-93-4 methyl (Z)-{4,4-difluoro-1-[4-(3-methylfuran-2-carbonylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene}acetate 
• 168162-92-3 methyl (Z)-{4,4-difluoro-1-[4-(3-methylthiophene-2-carbonylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-5-ylidene}acetate 
• 168162-51-4 (Z)-{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

Synthesis and biological activity of novel 4,4-difluorobenzazepine derivatives as non-peptide antagonists of the arginine vasopressin V 1A receptor

To find potent and selective antagonists of the arginine vasopressin (AVP) V1A receptor, optimization studies of compounds structurally related to (Z)-N-{4′-[(4,4-difluoro-5-carbamoylmethylidene-2,3,4,5-tetrahydro-1H- 1-benzazepin-1-yl)carbonyl

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.