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离体大鼠肝脏灌流法制备氯吡格雷活性巯基代谢物
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| 篇名： | 离体大鼠肝脏灌流法制备氯吡格雷活性巯基代谢物 |
| TITLE： | Preparation of active thiol metabolite of clopidogrel by isolated rat liver perfusion |
| 摘要： | 目的 建立氯吡格雷活性巯基代谢物（CATM）的制备方法，为顺式CATM的合成提供参考。方法以（S）-2-氧氯吡格雷为底物，采用离体大鼠肝脏灌流法和ChromCore120C18制备柱制备并分离纯化CATM。采用质谱和核磁共振氢谱鉴定目标产物，对比人体内活性构型（顺式CATM）保留时间确认目标产物中活性构型的占比。结果目标产物的转化率为11.71％，质谱和核磁共振氢谱鉴定目标产物为CATM。CATM的峰2～峰5为4个立体异构体，保留时间分别为21.3、22.3、26.5、27.3min，峰面积占比分别为7.13％、7.23％、63.52％、14.97％。根据人体内CATM活性构型的保留时间为26.3min，确定目标产物CATM中活性顺式异构体占比为63.52％。结论本方法成本低、步骤简单，可制备出活性构型占比较高的CATM。 |
| ABSTRACT： | OBJECTIVE To estab lish the pre paration method of clopidogrel active thiol metabolite （CATM），and to provide reference for the synthesis of cis-CATM. METHODS CATM was prepared ，separated and purified with isolated rat liver perfusion and ChromCore 120 C18 preparative column ，using（S）-2-oxo-clopidogrel as substrate. The target compounds were identified by mass spectrometry and nuclear magnetic resonance spectroscopy. The retention time of the active configuration of CATM in the human body （cis-CATM）were compared to confirm the proportion of active configuration in the target product. RESULTS The conversion rate of the target product was 11.71％. The target products were identified as CATM by MS and 1H-NMR. Peak 2-peak 5 of CATM were four stereoisomers. The retention time of them were 21.3，22.3，26.5，27.3 min. The peak area ratios of them were 7.13％，7.23％，63.52％，14.97％，respectively. Based on that retention time of the active configuration of CATM in human body was 26.3 min，the active cis-stereoisomer in the target product CATM accounted for 63.52％. CONCLUSIONS This method is low-cost ，simple，and can prepare CATM with higher active configuration. |
| 期刊： | 2022年第33卷第14期 |
| 作者： | 刘艺，陶婷，刘云，李艳丽，胡盼盼，姜艳娇，孙增先 |
| AUTHORS： | LIU Yi，TAO Ting，LIU Yun，LI Yanli，HU Panpan ，JIANG Yanjiao ，SUN Zengxian |
| 关键字： | 离体大鼠肝脏灌流；氯吡格雷；活性巯基代谢物；制备；纯化；（S）-2-氧氯吡格雷 |
| KEYWORDS： | isolated rat liver perfusion ；clopidogrel；active thiol me tabolite；preparation；purification；（S）-2-oxo-clopidogrel |
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