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Azasetron hydrochloride

Azasetron hydrochloride Structure
Azasetron hydrochloride structure
CAS No.
123040-69-7
Chemical Name:
Azasetron hydrochloride
Synonyms
Y-25130;AZASETRON HCL;Azasetron base;Arazasetron HCl;Azasetron Impurity?2;Y-25130 HYDROCHLORIDE;Azastron hydrochloride;Azasetron hydrochlorid;Azasetron hydrochloride;Azasetron hydrochloride base
CBNumber:
CB6675310
Molecular Formula:
C17H20ClN3O3
Molecular Weight:
349.81
MDL Number:
MFCD00209913
MOL File:
123040-69-7.mol
Last updated:2023-05-06 17:15:42
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Azasetron hydrochloride Properties

Melting point 301-303°C
Boiling point 558.0±50.0 °C(Predicted)
Density 1.42±0.1 g/cm3(Predicted)
storage temp. -20°C Freezer
pka 13.31±0.20(Predicted)
CAS DataBase Reference 123040-69-7(CAS DataBase Reference)
FDA UNII 77HC7URR9Z

Azasetron hydrochloride price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC A802805 Azasetron 123040-69-7 25mg $370 2021-12-16 Buy
AK Scientific L995 Azasetron 123040-69-7 50mg $404 2021-12-16 Buy
Biosynth Carbosynth FA18062 Azasetron hydrochloride 123040-69-7 10mg $75 2021-12-16 Buy
Biosynth Carbosynth FA18062 Azasetron hydrochloride 123040-69-7 50mg $262.5 2021-12-16 Buy
AvaChem 1699B Azasetron 123040-69-7 10mg $79 2021-12-16 Buy
Product number Packaging Price Buy
A802805 25mg $370 Buy
L995 50mg $404 Buy
FA18062 10mg $75 Buy
FA18062 50mg $262.5 Buy
1699B 10mg $79 Buy

Azasetron hydrochloride Chemical Properties,Uses,Production

Chemical Properties

White to Off-White Solid

Originator

Azasetron,Pharm Chemical

Uses

As a 5-HT3 receptor antagonist, Azasetron hydrochloride can be used as an antiemetic.

Definition

ChEBI: Azasetron hydrochloride is a benzoxazine.

Manufacturing Process

To a solution of 2-(2-carboxy-4-chlorophenoxy)acetic acid in concentrated sulfuric acid is added dropwise a mixed liquid of fuming nitric acid and concentrated sulfuric acid under stirring with keeping at a temperature below 10°C. After the addition, the reaction mixture is stirred and poured into 10 L of ice-cold water. The precipitated crystals are collected by filtration, washed with 2 L of water four times and them dried to give 2-(2-carboxy-4-chloro-6- nitrophenoxy)acetic acid.
To a solution of ferrous sulfate heptahydrate in of hot water is added a solution of 2-(2-carboxy-4-chloro-6-nitrophenoxy)acetic acid and aqueous concentrated ammonia solution in water under stirring. After stirring, to the reaction mixture is twice added aqueous concentrated ammonia solution. While the reaction mixture becomes exothermic, stirring is continued. The resultant mixture is filtered through a celite layer under reduced pressure and washed with hot water twice. The filtrate is cooled and made acid with concentrated hydrochloric acid. The precipitated crystals are washed with water and dried to give 6-chloro-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-8- carboxylic acid.
A mixture of 6-chloro-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-8-carboxylic acid, methanol and concentrated sulfuric acid is refluxed under heating with stirring, and then cooled. The precipitated crystals are collected by filtration, washed with methanol and dried to give methyl 6-chloro-3,4-dihydro-3-oxo- 2H-1,4-benzoxazine-8-carboxylate, melting point 239°-241°C.
To a solution of methyl 6-chloro-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-8-carboxylate in dimethylformamide is added potassium t-butoxide and solution stirred at room temperature. To the resultant solution is added dropwise a solution of methyl iodide in dimethylformainide under stirring. After the reaction solution is stirred, water is added thereto. The insoluble substance is collected by filtration, washed with water and dried to give methyl 6-chloro- 3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxylate. A mixture of methyl 6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4- benzoxazine-8-carboxylate, ethanol and 4% aqueous potassium hydroxide solution is refluxed with heating. The resultant solution is cooled and water is added thereto followed by filtration. The filtrate is made acid with concentrated hydrochloric acid. The precipitated crystals are collected by filtration, washed with water and dried, and then recrystallized from ethanol to give 6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxylic acid, melting point 241°-243°C.
A solution of 6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8- carboxylic acid in tetrahydrofuran and dimethylformamide is cooled to below 0°C and triethylamine is added under stirring thereto. Further, ethyl chlorocarbonate is added and the mixture is stirred at room temperature. To the resultant mixture is added 3-amino-8-azabicyclo[3.2.1]octane and the mixture stirred. After completion of the reaction, aqueous sodium hydrogen carbonate and ethyl acetate are added. The organic layer is separated, washed with water and dried over magnesium sulfate. The solvent is distilled off to give 6-chloro-3,4-dihydro-4-methyl-N-(8-azabicyclo[3.2.1]oct-3-yl)-3- oxo-2H-1,4-benzoxazine-8-carboxamide. In practice it is usually used as hydrochloride.

Therapeutic Function

Antiemetic

Azasetron hydrochloride Preparation Products And Raw materials

Raw materials

3-METHOXYPROPIONIC ACID 4-Methylmorpholine 3-Aminoquinuclidine Nitrification Chloroform
Chloroacetyl chloride Ammonium chloride Sodium bicarbonate Methyl 5-chloro-2-hydroxybenzoate Thionyl chloride
Iodomethane 8-Azabicyclo[3.2.1]octan-3-amine(9CI) Ammonium nitrate Ethyl chloroformate Sulfuric acid
Hydrochloric acid Nitric acid Ammonia Potassium tert-butoxide Potassium hydroxide
Triethylamine

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Preparation Products

Azasetron hydrochloride Suppliers

Global( 169)Suppliers
Supplier Tel Email Country ProdList Advantage
Henan Tianfu Chemical Co.,Ltd. 		+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21695 55
career henan chemical co 		+86-0371-86658258 sales@coreychem.com China 29914 58
Chongqing Chemdad Co., Ltd 		+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 47465 58
Shaanxi Dideu Medichem Co. Ltd 		+86-29-87569265 +86-18612256290 1056@dideu.com China 3842 58
Xi'an Yutbon Pharmaceutical Technology Co., Ltd 		029-81140587 +8618717328141 sales@yutbon.com China 437 58
SIMAGCHEM CORP 		+86-13806087780 sale@simagchem.com China 17367 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 29576 58
AFINE CHEMICALS LIMITED 		0571-85134551 info@afinechem.com CHINA 15377 58
Supplier Advantage
Henan Tianfu Chemical Co.,Ltd. 		55
career henan chemical co 		58
Chongqing Chemdad Co., Ltd 		58
CONIER CHEM AND PHARMA LIMITED 		58
Shaanxi Dideu Medichem Co. Ltd 		58
Xi'an Yutbon Pharmaceutical Technology Co., Ltd 		58
SIMAGCHEM CORP 		58
TargetMol Chemicals Inc. 		58
Dideu Industries Group Limited 		58
AFINE CHEMICALS LIMITED 		58

View Lastest Price from Azasetron hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Azasetron hydrochloride pictures 2022-09-30 Azasetron hydrochloride
123040-69-7
 US $0.00-0.00 / kg 1kg 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
Azasetron hydrochloride pictures 2021-09-29 Azasetron hydrochloride
123040-69-7
 US $0.00 / Kg/Bag 1KG 98%min 500kgs WUHAN FORTUNA CHEMICAL CO., LTD
Azasetron hydrochloride USP/EP/BP pictures 2021-08-05 Azasetron hydrochloride USP/EP/BP
123040-69-7
 US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited

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N-1-AZABICYCLO[2.2.2]-OCT-3-YL-6-CHLORO-3,4-DIHYDRO-4-METHYL-3-OXO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE, HYDROCHLORIDE N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HCL N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HYDROCHLORIDE Y-25130 Y-25130 HYDROCHLORIDE AZASETRON HCL Azasetron hydrochloride Azasetron base 6-chloro-3-keto-4-methyl-N-quinuclidin-3-yl-1,4-benzoxazine-8-carboxamide N-(1-azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide Azastron hydrochloride 3,4-DIHYDRO-4-METHYL-3-OXO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE, HYDROCHLORIDE Azasetron hydrochloride base Azasetron hydrochloride N-1-Azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxamide hydrochloride Azasetron hydrochlorid N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide hydrochloride Arazasetron HCl Azasetron hydrochloride USP/EP/BP Azasetron Impurity?2 123040-69-7 123040697 C17H20ClN3O3 C17H202N3O3HCl C17H20ClN3O3HCl Intermediates & Fine Chemicals Pharmaceuticals anti-emetic Active Pharmaceutical Ingredients