ChemicalBook > CAS DataBase List > Mozavaptan

Mozavaptan

Product Name
Mozavaptan
CAS No.
137975-06-5
Chemical Name
Mozavaptan
Synonyms
CS-134;OPC31260l;OPC 31260;MOZAVAPTAN;Mozavaptan USP/EP/BP;Mozavaptan (OPC-31260);N-(4-(5-(Dimethylamino);OPC-31260; OPC31260L; OPC 31260;-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl);5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine
CBNumber
CB51388577
Molecular Formula
C27H29N3O2
Formula Weight
427.54
MOL File
137975-06-5.mol
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Mozavaptan Property

Melting point:
213 - 217°C
Boiling point:
543.0±50.0 °C(Predicted)
Density 
1.21±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Room Temperature
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
13.04±0.70(Predicted)
color 
White to Off-White
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
M732720
Product name
Mozavaptan
Packaging
5mg
Price
$130
Updated
2021/12/16
ApexBio Technology
Product number
B2299
Product name
Mozavaptan
Packaging
10mg
Price
$95
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD71413
Product name
5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine
Packaging
100mg
Price
$120
Updated
2021/12/16
ChemScene
Product number
CS-6286
Product name
Mozavaptan
Purity
99.89%
Packaging
10mg
Price
$60
Updated
2021/12/16
ChemScene
Product number
CS-6286
Product name
Mozavaptan
Purity
99.89%
Packaging
50mg
Price
$180
Updated
2021/12/16
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Mozavaptan Chemical Properties,Usage,Production

Description

Mozavaptan is an oral vasopressin V2 antagonist that has been launched in Japan for inappropriate antidiuretic hormone secretion syndrome (IADHS), an affliction manifesting as hyponatremia. It joins another nonpeptidic benzazepine, conivaptan, which corrects sodium and water imbalance by blocking the renal V2 receptor resulting in enhanced diuresis, thereby effectively increasing serum sodium concentration. While conivaptan inhibits both V1 and V2 receptors, mozavaptan is significantly more selective for V2 (IC50 of 14nM vs. 1.2 mM for V1).

Originator

Otsuka (Japan)

Uses

Mozavaptan is a vasopressin-receptor antagonist. It is used in the treatment of congestive heart failure and hyponatremia.

Uses

vasopressin V2 receptor antagonist

Definition

ChEBI: Mozavaptan is a member of benzamides.

brand name

Physuline

Synthesis

The reported synthesis of mozavaptan is shown in the scheme. Readily available benzazepin-5-one 39 was refluxed with 40% methyl amine methanol solution in the presence of molecular sieves for 5h followed by the reduction of the resulting imine with sodium borohydride to give the monomethyl amine. Reductive alkylation of the monomethyl amine with formaldehyde in the presence of sodium cyanoborohydride gave the dimethyl amino benzazepine 40. Removal of the tosyl group was facilitated by heating 40 in polyphosphoric acid at 150oC for 2 h to give 41 in 97% yield. Reaction of the resulting benzazepine 41 with p-nitrobenzoyl chloride (42) in the presence of triethylamine provided amide 43 which was hydrogenated in the presence of 10% Pd/C in ethanol at room temperature to give aniline 44. Acylation of aniline 44 with 2-methylbenzoylchloride (45) in the presence of triethylamine gave mozavaptan (VI) in 54% yield.

Mozavaptan Preparation Products And Raw materials

Raw materials

Preparation Products

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Mozavaptan Suppliers

China 117 France 1 Germany 1 India 1 United Kingdom 1 United States 16 Global 137
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View Lastest Price from Mozavaptan manufacturers

Hebei Guanlang Biotechnology Co., Ltd.
Product
Mozavaptan 137975-06-5
Price
US $10.00/PCS
Min. Order
1KG
Purity
99%
Supply Ability
10 mt
Release date
2021-03-12
Hebei Mojin Biotechnology Co., Ltd
Product
Mozavaptan 137975-06-5
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
50000KG/month
Release date
2023-09-05
Zhuozhou Wenxi import and Export Co., Ltd
Product
Mozavaptan 137975-06-5
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10

137975-06-5, MozavaptanRelated Search:

Pyrazine (S)-(+)-Benzyl glycidyl ether Iodobenzene N-ACETYL-L-TYROSINE ETHYL ESTER β-Lonone 3-Hydroxypyridine Pyrrolidine Indoline Isoquinoline Tolvaptan Pidotimod Mozavaptan 2,3,4,5-Tetrahydro-1H-benzo[b]azepine 2,3,4,5-TETRAHYDRO-1H-BENZO[B]AZEPIN-5-YLAMINE N-{4-[(methylamino)methyl]phenyl}acetamide 4-amino-N-(2-ethylphenyl)benzamide 4-AMINO-N-ETHYL-N-PHENYLBENZAMIDE Mozavaptan Hydrochloride

  • OPC 31260
  • MOZAVAPTAN
  • 5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine
  • Benzamide, N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-
  • -2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)
  • N-(4-(5-(Dimethylamino)
  • CS-134
  • OPC-31260; OPC31260L; OPC 31260
  • OPC31260l
  • N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-
  • Mozavaptan USP/EP/BP
  • N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
  • N-(4-(5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)phenyl)-2-methylbenzamide
  • Mozavaptan (OPC-31260)
  • 137975-06-5
  • Inhibitors
  • Pharmaceutical intermediate