137976-61-5

Basic information

• Product Name: 2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide
• Synonyms: 2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide
• CAS NO: 137976-61-5
• Molecular Formula: C₂₅H₂₂N₂O₃
• Molecular Weight: 398.45378
• Mol File: 137976-61-5.mol

Chemical Properties

• Boiling Point: 553.103 °C at 760 mmHg
• Flash Point: 288.307 °C
• Appearance: /
• Density: 1.27
• CAS DataBase Reference: 2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide(CAS DataBase Reference)
• NIST Chemistry Reference: 2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide(137976-61-5)
• EPA Substance Registry System: 2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide(137976-61-5)

Safety Data

• Hazardous Substances Data: 137976-61-5(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2-Methyl-N-[4-[(2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]phenyl]benzamide is used as a potential pharmaceutical agent for [application reason]. Its unique chemical structure allows for possible interactions with biological targets, which could be harnessed for therapeutic purposes. Further research and development are required to explore its full potential and establish its efficacy in treating specific medical conditions.

Upstream product

• 118-90-1 ortho-methylbenzoic acid 
• 137976-09-1 1-(4-aminobenzoyl)-2,3,4,5-tetrahydro1H-1-benzazepin-5-one 
• 122-04-3 4-nitro-benzoyl chloride 
• 137975-89-4 1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one 
• 933-88-0 ortho-toluoyl chloride 
• 1127-74-8 1,2,3,4-tetrahydro-5H-benzo[b] azepin-5-one 

Downstream Products

• 150681-95-1 (Methyl-{1-[4-(2-methyl-benzoylamino)-benzoyl]-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl}-amino)-acetic acid ethyl ester 
• 150681-17-7 N-[4-(5-Amino-2,3,4,5-tetrahydro-benzo[b]azepine-1-carbonyl)-phenyl]-2-methyl-benzamide 
• 222541-11-9 ethyl (E)-<1-<4-(2-methylbenzoylamino)benzoyl>-2,3,4,5-tetrahydro-1H-1-benzoazepin-5-ylidene>acetate 
• 150681-19-9 5-hydroxy-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 154890-02-5 5-methylamino-1-[4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine 
• 222541-19-7 (E)-N-methyl-<1-<4-(2-methylbenzoylamino)benzoyl>-2,3,4,5-tetrahydro-1H-1-benzoazepin-5-ylidene>acetamide 

Relevant articles and documents

Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form

The anti and syn isomers of tolvaptan-type compounds, N-benzoyl-5-hydroxy-1-benzazepines (5a-c), were prepared in a stereocontrolled manner by biasing the conformation with a methyl group at C9 and C6, respectively, and the enantiomeric forms were separat

Nonpeptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 4'-[5-(substituted methylidene)-2,3,4,5-tetrahydro-1H-1-benzoazepine-1-carbonyl]benzanilide and 4'-[5-(substituted methyl)-2,3-dihydro-1H-1-benzoazepine-1- carbonyl]benzanilide derivatives

Arginine vasopressin (AVP) has a dual action, i.e. vasoconstriction and water reabsorption via V(1A) and V2 receptors, and may play a role in a number of diseases, including congestive heart failure (CHF), hypertension, renal disease, edema, and hyponatremia. We have attempted to develop a new series of AVP antagonists for both V(1A) and V2 receptors based on the hypothesis that the blockade of both V(1A) and V2 receptors might be beneficial to CHF patients. In this report, a series of compounds structurally related to 4'-[5-(substituted methylidene)2,3,4,5-tetrahydro- 1H-1-benzoazepine-1-carbonyl]benzanilide (exo-olefin isomer) and 4'-[5- (substituted methyl)2,3-dihydro-1H-1-benzoazepine-1-carbonyl]benzanilide (endo-olefin isomer) were synthesized and examined to have AVP antagonist activity for both V(1A) and V2 receptors. As a result, it was found that the (E)-exo-olefin isomers showed more potent binding affinity compared with endo-olefin isomers. Among these (E)-exo-olefin isomers, (E)-N-methyl-{1- [4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzoazepin-5- ylidene}ac-etamide (14) exhibited the most potent binding affinitiy and (E)- N-methyl-(1-{4-12-(4'methylphenyl)benzoyl-amino]benzoyl}-2,3,4,5- tetrahydro-1H-1-benzoazepin-5-ylidene)acetamide (20) exhibited a high AVP antagonist activity for both V(1A) and V2 receptors after intravenous administration. Details of the synthesis and pharmacological properties of this series are presented.

Condensed benzazepine derivative and pharmaceutical composition thereof

This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) STR1 (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R1 and R2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group, A: a single bond; a group represented by the formula n: 0 or an integer of from 1 to 3, R3 and R4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R3 and R4 may together form a lower alkylene group having 2 to 7 carbon atoms), and ring C: a benzene ring which may optionally have substituent(s)) and salts thereof; to pharmaceutical compositions which contain these compounds as an active ingredient and to intermediates which are useful in synthesizing these compounds. The compounds of this invention are useful as arginine vasopressin antagonists.

Orally active, nonpeptide vasopressin V2 receptor antagonists: A novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds

This paper describes a novel series of nonpeptide vasopressin V2 receptor antagonists. It has been demonstrated that the 1-[4- (benzoylamino)benzoyl]-2,3,4,5-1H-benzazepines and 1-[4- (benzoylamino)benzoyl]-2,3,4,5-1H-1,5-benzodiazepines show a high affinity for V2 (and V(1a)) receptors. Among the 1-[4-(benzoylamino)benzoyl]-2,3,4,5- 1H-benzazepine series, compounds with an alkylamino group on the benzazepine ring have been shown to have oral activity. A lipophilic group at the ortho position on the terminal benzoyl ring is important for both high V2 receptor affinity and oral activity. On the basis of these favorable properties, clinical testing of 31b has begun for use as an oral and iv aquaretic agent.