| 巯基化阿霉素的两种合成方法的比较 |
| 投稿时间：2014-08-02 修订日期：2014-10-13 点此下载全文 |
| 引用本文：吴珊,张叶叶,郭海霞,刘俊杰,孙治国,钟延强,邹豪.巯基化阿霉素的两种合成方法的比较[J].药学实践杂志,2014,32(6):428~433 |
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| 基金项目:国家自然科学基金项目(30801441);科技部重大新药创制专项(2014ZX09J14107-01B). |
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| 中文摘要:目的 探索合成供金纳米粒载药系统研究用模型药物巯基化阿霉素的可行方法。方法 分别采用2-亚氨基硫烷盐酸盐(2-IT)法和琥珀酰亚胺-S-乙酰基硫代乙酸酯(SATA)法合成巯基阿霉素,通过高效液相色谱(HPLC)、飞行时间质谱(MS-ESI)及核磁共振氢谱(1H NMR)验证巯基阿霉素的合成,并考察反应物摩尔比、反应时间等因素对合成巯基阿霉素的影响。结果 1H NMR 确证DOX-SATA出现了与硫酯基团相连的质子信号,表明新合成的化合物中含有硫酯基团。HPLC及MS-ESI结果显示,两种方法均能合成巯基阿霉素,2-IT法生成的巯基阿霉素,随着反应时间延长易发生环化,形成环化巯基阿霉素。SATA试剂法合成巯基阿霉素过程中不易发生副反应,合成的巯基阿霉素较为稳定。结论 通过两种方法的比较,SATA法合成巯基阿霉素的方法较为可行。 |
| 中文关键词:巯基化阿霉素 2-亚氨基硫烷盐酸盐(2-IT) 琥珀酰亚胺-S-乙酰基硫代乙酸酯(SATA) |
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| A comparison study of synthesizing methods of thiolated doxorubicin |
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| Abstract:Objective To investigate the optimal method for synthesizing thiolated doxorubicin.Methods Thiolated doxorubicin was synthesized through two different methods. Doxorubicin was reacted with 2-iminothiolane (2-IT) and S-acetylthioglycolic acid N-hydroxysuccinimide ester (SATA),respectively. The synthesized thiolated doxorubicin was further characterized by HPLC and MS-ESI techniques. Several factors including molar ratios as well as reaction time were evaluated.Results The results showed that thiolated doxorubicin could be synthesized via both of the two methods successfully. Thiolated doxorubicin could be stable when doxorubicin was reacted with SATA. But the crude thiolated doxorubicin could be cyclized easily when doxorubicin was reacted with 2-IT.Conclusion Thiolated doxorubicin prepared with SATA is more feasible than that with 2-IT. |
| keywords:thiolated doxorubicin 2-iminothiolane (2-IT) S-acetylthioglycolic acid N-hydroxysuccinimide ester (SATA) |
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