| 摘要: |
| 目的 合成利伐沙班的3个降解杂质，从而加强对Xa因子抑制剂类抗凝药利伐沙班原料药的质量控制。方法 利伐沙班（1）经开环反应得到杂质A；杂质A经水解反应得到杂质B；杂质A经取代反应得到杂质C。结果 合成的3种降解杂质的结构经1H-NMR、13C-NMR和MS确证，纯度经HPLC检测均>99.0%。结论 3个杂质可作为利伐沙班原料药质量控制的杂质对照品。 |
| 关键词: 利伐沙班 降解杂质 合成 |
| DOI：10.13748/j.cnki.issn1007-7693.2017.05.014 |
| 分类号:R914.5 |
| 基金项目: |
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| Synthesis of the Degradation Impurity of Rivaroxaban |
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PENG Jiaxun1, MAO Yu2
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1.Hunan Institute of Engineering, Xiangtan 411101, China;2.Changsha Rongguangda Biological Technology Co., Ltd., Changsha 410013, China
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| Abstract: |
| OBJECTIVE To perform the quality of rivaroxaban which was a kind of anticoagulant drug, three degradation impurities A, B and C were synthesized and characterized. METHODS Rivaroxaban (1 ) was used as starting material to prepare Impurity A , impurity B was synthesized by hydrolyzing impurity A , and impurity C was obtained from impurity A by substitution reaction. RESULTS The structures of the three impurities had been verified by 1H-NMR and 13C-NMR and MS. Their purities were over 99.0% (detected by HPLC). CONCLUSION The synthetic degradation impurities can be used as the reference substance of the impurities in the quality control of rivaroxaban. |
| Key words: rivaroxaban degradation impurity synthesis |
