| 瑞加德松的全合成研究 |
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| 引用本文： | 刘伟,罗剑飞,张志刚.瑞加德松的全合成研究[J].上海医药,2016(3):73-75. |
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| 作者姓名： | 刘伟 罗剑飞 张志刚 |
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| 作者单位： | 上海紫源制药有限公司 上海 201108 |
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| 摘 要： | 目的：改进瑞加德松的合成工艺，提高收率与质量，获得良好的生产工艺。方法：以2-氯腺苷的羟基为原料，经叔丁基二甲基硅烷保护，与水合肼反应得2’,3’,5’-三叔丁基二甲基硅氧基-2-肼基腺苷，再和2-甲酰基-3-氧代丙酸乙酯环合后经甲胺化得带保护的瑞加德松，最后脱去保护基得到瑞加德松。结果：产品纯度和收率分别提高到99.0%和47.2%。结论：优化后工艺收率高，产品质量好，操作简便，适合工业化生产。
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| 关 键 词： | 瑞加德松 合成 工艺改进 纯化 |
Total synthesis of regadenoson |
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| Abstract: | Objective: To improve the process for the synthesis of regadenoson and its quality.Methods:Regadenoson was synthesized from 2-chloroadenosine via etheriifcation with t-butyldimethylchlorosilane, reaction with hydrazine hydrate to give 2’,3’,5’-tri-(tert-butyldimethylsiyl)oxy-2-hydrazinyl adenosine, which was cyclized with ethyl 2-formyl-3-oxopropanoate, and ifnally the protecting groups were removed.Results: The purity and yield of regadenoson were improved up to 99.0% and 47.2%, respectively.Conclusion:The improved process can be easily operated with high yield and quality, and is suitable to industrial production. |
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| Keywords: | regadenoson synthesis process improvement puriifcation |
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