| 10-羟基喜树碱水溶性磷酰化衍生物的合成 |
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| 引用本文： | 杨柳,徐春艳,贾梦秋. 10-羟基喜树碱水溶性磷酰化衍生物的合成[J]. 过程工程学报, 2006, 6(6): 912-916 |
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| 作者姓名： | 杨柳 徐春艳 贾梦秋 |
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| 作者单位： | 北京化工大学材料科学与工程学院,北京,100029;北京化工大学材料科学与工程学院,北京,100029;北京化工大学材料科学与工程学院,北京,100029 |
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| 摘 要： | 以10-羟基喜树碱(HCPT)为原料，吡啶为溶剂，经过磷酰化、酯化、水解三步反应合成了全新的水溶性磷酰化衍生物. 得到的较佳工艺条件为：磷酰化反应三氯氧磷与HCPT的投料摩尔比2:1(相对0.01 mol HCPT)，反应温度-10℃，搅拌下反应时间30 min；酯化反应乙醇与HCPT的投料摩尔比6:1，反应温度10℃，搅拌下反应时间1.5 h；水解反应保持体系pH<5.0. ODS制备柱分离得到产物，总收率为30.0%.
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| 关 键 词： | 10-羟基喜树碱 磷酰化 合成 衍生物 |
| 文章编号： | 1009-606X（2006）06-0912-05 |
| 收稿时间： | 2005-12-20 |
| 修稿时间： | 2005-12-202006-01-23 |
Synthesis of New Water-soluble 10-Hydroxycamptothecin Derivative |
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| YANG Liu,XU Chun-yan,JIA Meng-qiu. Synthesis of New Water-soluble 10-Hydroxycamptothecin Derivative[J]. Chinese Journal of Process Engineering, 2006, 6(6): 912-916 |
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| Authors: | YANG Liu XU Chun-yan JIA Meng-qiu |
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| Affiliation: | College of Materials Science and Engineering, Beijing University of Chemical Technology |
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| Abstract: | Water-soluble derivative with the lactone ring intact was synthesized by using 10-hydroxycamptothecin (HCPT) as raw material and pyridine as solvent through phosphorylation, esterification and hydrolysis. The optimal reaction conditions for the phosphorylation were determined as follows: n(POCl3):n(HCPT)=2:1 (based on 0.01 mol HCPT), the reaction temperature -10℃, and the reaction time 30 min under stirring, for the esterification they are: n(ethanol):n(HCPT)=6:1, the reaction temperature 10℃, and the reaction time 1.5 h under stirring, pH<5.0 in hydrolysis reaction. The product, 10-hydroxycamptothecin derivative, was separated by octodecyl silica gel preparative column. The total yield of the derivative was 30%. |
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| Keywords: | 10-hydroxyeamptothecin phosphorylation synthesis derivative |
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