| 磺达肝癸钠甲苷单糖中间体的合成工艺改进研究 |
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| 引用本文： | 孙福亮,韩健,常淑梅,侯文锋,李振重,袁海新,干浩. 磺达肝癸钠甲苷单糖中间体的合成工艺改进研究[J]. 现代药物与临床, 2016, 31(3): 269-272. DOI: 10.7501/j.issn.1674-5515.2016.03.001 |
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| 作者姓名： | 孙福亮 韩健 常淑梅 侯文锋 李振重 袁海新 干浩 |
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| 作者单位： | 天津红日药业股份有限公司,天津,301700 |
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| 基金项目： | 天津市科技计划项目(13ZCZDSY00600) |
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| 摘 要： | 目的对磺达肝癸钠中单糖中间体的合成工艺进行改进研究。方法以D-氨基葡萄糖为起始原料,经甲苷反应、苄基化反应得到单糖中间体。结果得到了α构型磺达肝癸钠甲苷单糖片段产物,HPLC检测质量分数可达98%以上,总收率为41.2%。结论磺达肝癸钠甲苷单糖中间体的合成工艺可简化操作,降低成本,提高安全性,方便生产。
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| 关 键 词： | 磺达肝癸钠 甲苷反应 α β异构体 |
| 收稿时间： | 2015-11-17 |
Improvement of method for synthesis of methyl glucosamine intermediate of fondaparinux sodium |
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| SUN Fu-liang,HAN Jian,CHANG Shu-mei,HOU Wen-feng,LI Zhen-zhong,YUAN Hai-xin and GAN Hao. Improvement of method for synthesis of methyl glucosamine intermediate of fondaparinux sodium[J]. Drugs & Clinic, 2016, 31(3): 269-272. DOI: 10.7501/j.issn.1674-5515.2016.03.001 |
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| Authors: | SUN Fu-liang HAN Jian CHANG Shu-mei HOU Wen-feng LI Zhen-zhong YUAN Hai-xin GAN Hao |
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| Affiliation: | Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China;Tianjin Chasesun Pharmaceutical Co., Ltd., Tianjin 301700, China |
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| Abstract: | Objective To study the improved method for synthesis of methyl glucosamine intermediate of fondaparinux sodium. MethodsD-Glucosamine was used as starting material to synthesize the target compound by methyl glycosylation and benzylation.Results The methylα-glucosamine intermediate of fondaparinux sodium was synthesized. The purity reaches above 98% by HPLC, and the total yield was 41.2%.Conclusion The synthetic technology of methyl glucosamine intermediate of fondaparinux sodium can simplify the operation, reduce the cost, improve the safety, and is convenient for production. |
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| Keywords: | fondaparinux sodium methyl glycosylation α,β-anomers |
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