1478664-02-6
EzetiMibe (3R,4R,3'S)-IsoMer
CAS: 1478664-02-6
Molecular Formula: C24H21F2NO3
1478664-02-6 - Names and Identifiers
| Name | EzetiMibe (3R,4R,3'S)-IsoMer |
| Synonyms | Ezetimibe-25 (3'S,3R,4R)-Ezetimbe Ezetimibe Impurity F (3'S,3R,4R)-Ezetimibe (3R,4R,3'S)-Ezetimibe EzetiMibe (3R,4R,3'S)-IsoMer (3R,4R)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one |
| CAS | 1478664-02-6 |
1478664-02-6 - Physico-chemical Properties
| Molecular Formula | C24H21F2NO3 |
| Molar Mass | 409.43 |
| Density | 1.334±0.06 g/cm3(Predicted) |
| Boling Point | 654.9±55.0 °C(Predicted) |
| pKa | 9.72±0.30(Predicted) |
1478664-02-6 - References
| Background | ezetimibe (3R,4R,3's) isomer is ezetimibe impurity L. Ezetimibe (Ezetimibe) was developed by Schering-Plough (Schering-Plough) company. Ezetimibe was approved by FDA in 102012, and was first launched in Germany in 11of the same year under the trade name Ezetrol. Ezetimibe is the first selective cholesterol absorption inhibitor, which can interfere with the absorption of food-derived cholesterol and cholesterol synthesized by the liver in the enterohepatic circulation, the absorption of other nutrients does not affect. |
| Application | ezetimibe (3R,4R,3 's) isomer is ezetimibe impurity L. Mainly used in laboratory research and development process and chemical and pharmaceutical production process. |
| preparation | add 54mL of DCM and 10.0g of compound ezetimibe to the reaction flask, stir at room temperature for 10~30min, add 15.0g of BSA to the reaction flask, and react at 20~50 °c for 1~2H, add 30.0G of MTBE to the reaction flask, after stirring for 30-60min at this temperature, 7.5g of BSA was added to the reaction flask and stirred for 1-3H at 20-40 °c. 0.3g of TBA. 3h2o was dissolved in 6mL of DCM, and the solution was added dropwise to the reaction flask. After completion of the dropwise addition, the reaction was stirred at 10-30 °c for 1-2H. The reaction solution was concentrated to dryness, 40.0G of isopropanol was added to the concentrate, and the reaction was stirred at 10-30 °c for 30min. 1.0g of concentrated sulfuric acid was dissolved in 50.0G of purified water, and the prepared solution was slowly added dropwise to the reaction solution. After completion of the dropwise addition, the reaction was stirred at 20 to 30 ° C. For 1 hour. The temperature of the reaction flask was adjusted to 0 to 20 ° C., and the mixture was stirred for 1 to 2 hours under this condition, followed by filtration. The filter cake was washed with purified water, and then dried to obtain 8.6g of a crude impurity L(SRR). The yield was 95.3, the chemical purity was 91.2, and the chiral purity was 87.5. The obtained crude impurity L was dissolved in 70ml of acetone at 20-40 °c, and 70ml of purified water was slowly added dropwise to the reaction solution and stirred at 40 °c for 1H, the temperature was slowly lowered to 20 ° C., filtered, and dried to obtain 6.3g of a crude impurity L(SRR). The yield was 86.7, the chemical purity was 99.1, and the chiral purity was 98.6. Add 50ml of ethanol to the above-obtained 6.3g of crude product and dissolve under heating. Slowly add 68ml of purified water Dropwise to the reaction and stir at 40 °c for 1H, the temperature was slowly cooled to 20 ° C., stirred for 2H under this condition, filtered, and dried to obtain 5.8g of impurity L(SRR). The yield was 81.2, the chemical purity was 99.99, and the chiral purity was 100. |
Last Update：2024-04-09 21:04:16
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Product Name: Ezetimibe Impurity 4 Visit Supplier Webpage Request for quotationCAS: 1478664-02-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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