123039-99-6
Azasetron
CAS: 123040-93-7;123040-95-9;123039-99-6
Molecular Formula: C17H21Cl2N3O3
123039-99-6 - Names and Identifiers
123039-99-6 - Physico-chemical Properties
| Molecular Formula | C17H21Cl2N3O3 |
| Molar Mass | 386.27294 |
| Density | 1.42g/cm3 |
| Boling Point | 550.4°C at 760 mmHg |
| Flash Point | 286.6°C |
| Vapor Presure | 3.68E-12mmHg at 25°C |
| Refractive Index | 1.653 |
| Use | Used as an antineoplastic agent |
123039-99-6 - Nature
Open Data Verified Data
crystallization from an ethanolic solution of hydrogen chloride. Melting point 281 °c (decomposition). There is also crystallization from ethanol, melting point 305 ° C (decomposition).
Last Update：2024-01-02 23:10:35
123039-99-6 - Preparation Method
Open Data Verified Data
methyl 5 monochloro-2-hydroxybenzoate was nitrated with nitric acid in sulfuric acid solution and then reduced to amine with iron powder and ammonium chloride in water. The resulting amine and Chloroacetyl Chloride are acylated and cyclized in a mixture of chloroform and water under the action of sodium bicarbonate, and the resulting compound is methylated with methyl iodide in the presence of dimethyl formamide and potassium carbonate, and then hydrolyzed to a carboxylic acid. Then, it is refluxed with thionyl chloride to form acyl chloride, and finally, it is condensed with 3-aminoquinine in chloroform containing N-methylmorpholine to obtain azasetron.
Last Update：2022-01-01 09:23:26
123039-99-6 - Use
Open Data Verified Data
It was jointly developed by Japan Yoshitomi Pharn Inc. and Japan Tobacco Co., Inc. and was first launched in Japan in 1994. For the 5 serotonin type 3 (5-HT3) receptor antagonist antiemetic drugs. It has potent and selective antagonism of the 5-HT3 receptor without dopamine receptor antagonism. It is suitable for the treatment of Nausea, Vomit and other gastrointestinal symptoms caused by anti-malignant tumor drugs.
Last Update：2022-01-01 09:23:27
123039-99-6 - Safety
Open Data Verified Data
male rats, female rats intravenous injection LD50 (mg/kg):135, 132.
Last Update：2022-01-01 09:23:27
123039-99-6 - Reference Information
| Use | use as antineoplastic agent |
Last Update：2024-04-10 22:29:15
