159588-63-3

Upstream product

• 159588-56-4 1-pyridin-3-ylmethyl-1,3,4,5-tetrahydro-benzo[b][1,4]diazepin-2-one 
• 159588-58-6 1-(3-pyridyl)methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 
• 159588-60-0 (4-nitro-phenyl)-(5-pyridin-3-ylmethyl-2,3,4,5-tetrahydro-benzo[b][1,4]diazepin-1-yl)-methanone 
• 6959-48-4 3-chloromethylpyridinium chloride 
• 5755-07-7 2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one 

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.