159589-35-2

Upstream product

• 14002-52-9 o-phenylbenzoyl chloride 
• 159589-07-8 ethyl <5-(4-aminobenzoyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-1-yl>acetate 
• 6516-89-8 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 
• 122-04-3 4-nitro-benzoyl chloride 
• 947-84-2 2-Biphenylcarboxylic acid 
• 159589-06-7 [5-(4-nitro-benzoyl)-2,3,4,5-tetrahydro-benzo[b][1,4]diazepin-1-yl]-acetic acid ethyl ester 
• 159589-05-6 1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 

Downstream Products

• 159589-37-4 <5-<4-(2-phenylbenzoylamino)benzoyl>-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-1-yl>acetic acid 

Relevant academic research and scientific papers

Nonpeptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 2-phenyl-4'-(2,3,4,5- tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide derivatives

A series of compounds structurally related to 2-phenyl-4'-(2,3,4,5- tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V(1A) and V2 receptors. The introduction of a hydrophilic substituent group into the 5-position of the benzodiazepine ring resulted in an increase in oral availability. Especially, the (3-pyridyl)methyl (31b), the 2-(4- methyl)-1,4-diazepan-1-yl)-2-oxoethyl (32i), and the 2-(4-methylpiperazin-1- yl)ethyl (33g) derivatives exhibited high antagonist activities and high oral availability. Details of the synthesis and pharmacological properties of this series are presented.