| 引用本文: | 王永毅,冯锋,田连忠,王琼,喻琼林.半合成紫杉醇工艺杂质研究[J].中国现代应用药学,2014,31(2):154-158. |
| WANG Yongyi,FENG Feng,TIAN Lianzhong,WANG Qiong,YU Qionglin.Study on the Process-related Impurities of Semi-synthetic Paclitaxel[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(2):154-158. |
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| 摘要: |
| 目的 研究半合成紫杉醇工艺杂质，结合合成路线推测工艺杂质的来源。方法 利用硅胶柱色谱制备分离了kingston半合成路线中的4个工艺杂质，通过质谱及核磁共振波谱鉴定化学结构。结果 4个工艺杂质分别是5β,20-环氧-1,7β-二羟基-9-羰基紫杉-11-烯-2α,4,10β,13α-四取代基4,10-二乙酰氧基2-苯甲酰氧基13-[(2R,3S)]-3-氨基-2-苯甲酰氧基-3-苯基丙酸酯(1)、7-乙酰基紫杉醇(2)、13-Tes-巴卡亭Ⅲ(3)、7-表紫杉醇(4)。结论 杂质(1)尚未被美国药典和欧洲药典收载，研究结果为半合成紫杉醇的质量控制提供了依据。 |
| 关键词: 半合成紫杉醇 质量控制 工艺杂质 |
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| Study on the Process-related Impurities of Semi-synthetic Paclitaxel |
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WANG Yongyi1, FENG Feng2, TIAN Lianzhong1, WANG Qiong1, YU Qionglin1
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1.Jiangsu Yew Pharmaceutical Co., Ltd., Hodo Group, Wuxi 214199, China;2.China Pharmaceutical University, Nanjing 210009, China
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| Abstract: |
| OBJECTIVE To study the process-related impurities of semi-synthetic paclitaxel and discuss the formation mechanism according to the synthetic route. METHODS The process-related impurities of semi-synthetic paclitaxel in kingston route were isolated by silica gel column chromatography and identified by mass spectrometry and nuclear magnetic resonance analysis. RESULTS Their structures were 5β,20-epoxy-1,7β-dihydroxy-9-oxotax-11-ene-2α,4,10β, 13α-tetrayl 4, 10-diacetate 2-benzoate 13-[(2R,3S)]-3-amino-2-benzoate-3-phenylpropanaoate(1), 7-acetylpaclitaxel(2), 13-Tes-baccatin Ⅲ(3), 7-epipaclitaxel(4), respectively. CONCLUSION Impurity(1) has not been recorded by United States Pharmacopoeia and European Pharmacopoeia. The result could provide a basis for quality control of semi-synthetic paclitaxel. |
| Key words: semi-synthetic paclitaxel quality control impurity |
