ChemicalBook > CAS DataBase List > 5-Dehydro Tolvaptan

5-Dehydro Tolvaptan

Product Name: 5-Dehydro Tolvaptan
CAS No.: 137973-76-3
Chemical Name: 5-Dehydro Tolvaptan
Synonyms: Dehydrotolvaptan;5-Dehydro Tolvaptan;Tolvaptan Intermediate;Tolvaptan 5-Oxo Analog;Tolvaptan impurity 5 (DM-21826);7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-ox...;N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methy;N-[4-(7-chloro-5-oxo-3,4-dihydro-2H-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide;N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbe;7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine
CBNumber: CB72500620
Molecular Formula: C26H23ClN2O3
Formula Weight: 446.93
MOL File: 137973-76-3.mol

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5-Dehydro Tolvaptan Property

Melting point:: >118°C (dec.)
Boiling point:: 593.2±50.0 °C(Predicted)
Density: 1.307
storage temp.: Sealed in dry,Room Temperature
solubility: DMSO (Slightly), Methanol (Slightly)
form: Solid
pka: 12.97±0.70(Predicted)
color: White to Off-White
InChIKey: VENGMROMZOKURN-UHFFFAOYSA-N
SMILES: C(NC1=CC=C(C(N2C3=CC=C(Cl)C=C3C(=O)CCC2)=O)C(C)=C1)(=O)C1=CC=CC=C1C

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC

Product number: D230350
Product name: 5-DehydroTolvaptan
Packaging: 50mg
Price: $1190
Updated: 2021/12/16

Matrix Scientific

Product number: 096805
Product name: N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide
Purity: 95+%
Packaging: 1g
Price: $1647
Updated: 2021/12/16

Medical Isotopes, Inc.

Product number: 56358
Product name: 5-DehydroTolvaptan
Packaging: 50mg
Price: $2200
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FC151485
Product name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Packaging: 2mg
Price: $59
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FC151485
Product name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Packaging: 50mg
Price: $704
Updated: 2021/12/16

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5-Dehydro Tolvaptan Chemical Properties,Usage,Production

Uses

5-Dehydro Tolvaptan is an impurity of Tolvaptan (T536650), a selective, competitive arginine vasopressin V2 receptor antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH g

Preparation

To a 3 L reactor was added 1- (4-amino-2-methylbenzoyl) -7-chloro-5-oxo-2,3,4,5-tetrahydro- 1 H- 1 -benzazepine (70. 0 g, 212.90 mmol), dichloromethane (560 ml) and distilled water (140 ml), and the mixture was stirred for 1 hour. Magnesium hydroxide (14.90 g, 14.90 mmol) was added to the reaction mixture at 10 ° C. or lower, and the mixture was stirred for 30 minutes. 2-Methylbenzoyl chloride (30.42 ml) was gradually added to the reaction mixture, stirring for 3 hours. The reaction mixture was filtered to remove magnesium hydroxide, and the pH of the reaction mixture was adjusted to pH 8 to 9 using an aqueous sodium hydroxide solution, and then the organic layer was separated. The obtained organic layer was dried with sodium sulfate (Na 2 SO 4), filtered, and concentrated under reduced pressure to give 5-Dehydro Tolvaptan (yield: 96 percent).

Synthesis

933-88-0

137977-97-0

137973-76-3

To a 3 L reactor was added 1-(4-amino-2-methylbenzoyl)-7-chloro-3,4-dihydro-1H-benzo[b]azepin-5(2H)-one (70.0 g, 212.90 mmol), dichloromethane (560 mL), and distilled water (140 mL), and the reaction mixture was stirred for 1 hour. Magnesium hydroxide (14.90 g, 14.90 mmol) was slowly added to the reaction mixture at a temperature controlled below 10 °C and stirring was continued for 30 min. Subsequently, o-toluoyl chloride (30.42 mL) was slowly added dropwise and the reaction was continued with stirring for 3 hours after the dropwise addition. After completion of the reaction, the magnesium hydroxide was removed by filtration and the pH of the filtrate was adjusted to 8-9 with aqueous sodium hydroxide to separate the organic layer. The organic layer was dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure to afford 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine 91.35 g in 96% yield.

References

[1] Patent: JP2018/12690, 2018, A. Location in patent: Paragraph 0029; 0030
[2] Patent: CN105315169, 2016, A. Location in patent: Paragraph 0170; 0224; 0225
[3] Patent: CN105753735, 2016, A. Location in patent: Paragraph 0181; 0217; 0218
[4] Patent: CN106883175, 2017, A. Location in patent: Paragraph 0017; 0018
[5] Patent: CN108503586, 2018, A. Location in patent: Paragraph 0044; 0045; 0054; 0055; 0056

5-Dehydro Tolvaptan Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from 5-Dehydro Tolvaptan manufacturers

Guangzhou Tosun Pharmaceutical Ltd

Product: Tolvaptan Impurity 8 137973-76-3
Price: US $0.00-0.00/mg
Min. Order: 5mg
Purity: 95%+
Supply Ability: 1000mg
Release date: 2025-01-21

ShenZhen H&D Pharmaceutical Technology Co., LTD

Product: Tolvaptan Impurity 4 137973-76-3
Price: US $0.00-0.00/mg
Min. Order: 10mg
Purity: 98%
Supply Ability: 500mg
Release date: 2024-08-12

Cangzhou Wanyou New Material Technology Co.,Ltd

Product: Tolvaptan Intermediate 137973-76-3
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 5 tons
Release date: 2019-08-04

137973-76-3, 5-Dehydro TolvaptanRelated Search:

(R)-(+)-Tolvaptan Ethyl 7-Chloro-5-oxo-1-toxyl-2,3,4,5,-tetrahydro-1H-benzo[b]azepine-4-carboxylate Tolvaptan Impurity 18 Tolvaptan Impurity 13 5-Chloro-2-[(4-ethoxy-4-oxobutyl)[(4-methylphenyl)sulfonyl]amino]benzoic acid methyl ester Tolvaptan Impurity 21 Tolvaptan Impurity 3 (DM-4104) Tolvaptan Impurity 30 7-Chloro-1,2,3,4-tetrahydro-1-[(4-methylphenyl)sulfonyl]-5H-1-benzazepin-5-one Tolvaptan Impurity 17 Tolvaptan impurity 2 Tolvaptan Impurity 20 Tolvaptan Impurity 15 Tolvaptan Impurity 11 Tolvaptan Impurity 26 Tolvaptan 7-Chloro-1,2,3,4-tetrahydrobenzo(b)azepin-5-one 7-Chloro-1,2,3,4-tetrahydro-1-(2-methyl-4-nitrobenzoyl)-5H-1-benzazepin-5-one

N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide

7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine

N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbe

5-Dehydro Tolvaptan

N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-Methylphenyl)-2-MethylbenzaMide

Dehydrotolvaptan

N-[4-[7-Chloro-2,3,4,5-Tetrahydro-5-oxo-1H-1-Benzazepine-1-yl)carbonyl]-3-MethylPhenyl]-2-MethylBenzamide

N-[4-(7-chloro-5-oxo-3,4-dihydro-2H-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide

N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methy

Tolvaptan Intermediate

Tolvaptan impurity 5 (DM-21826)

Tolvaptan 5-Oxo Analog

Benzamide, N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-

N-[4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide

7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-ox...

N-[4-[(7- chloro -2,3,4,5- tetrahydro -5- oxo -1H-1- benzoazepine -1- yl) carbonyl ]-3- methylphenyl ]-2- methylbenzamide *

N-[4-[(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide

137973-76-3

Tolvaptan intermediate