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| 卡培他滨合成工艺改进 | |
| 引用本文： | 钟国琛,马祥. 卡培他滨合成工艺改进[J]. 安徽医药, 2010, 14(4): 395-396. DOI: 10.3969/j.issn.1009-6469.2010.04.011 |
| 作者姓名： | 钟国琛 马祥 |
| 作者单位： | 山东大学药学院,山东,济南,250012;安徽中医学院药学院,安徽,合肥,230031;山东大学药学院,山东,济南,250012 |
| 摘 要： | 目的分析比较卡培他滨的几种基本的合成路线。方法选择以1’，2’，3’-O-三乙酰基核糖为原料，经过缩合、酰化、水解合成卡培他滨的路线，在合成2’，3’-二乙酰-5’-脱氧-5-氟胞啶时用氢氧化钠替代碳酸氢钠中和。结果和结论可以减少碱用量，并减少成盐量，后处理方便；并对卡培他滨合成中的温度和碱浓度进行了考察，选择合适了的工艺条件，总收率达到68．1％。 |
| 关 键 词： | 核糖 胞苷 卡培他滨 工艺改进 |
Improved synthesis of Capecitabine |
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| ZHONG Guo-chen,MA Xiang. Improved synthesis of Capecitabine[J]. Anhui Medical and Pharmaceutical Journal, 2010, 14(4): 395-396. DOI: 10.3969/j.issn.1009-6469.2010.04.011 | |
| Authors: | ZHONG Guo-chen MA Xiang |
| Affiliation: | 1.School of Pharmaceutical Sciences;Shandong University;Jinan;Shandon 250012;2.Department of Pharmacy;Anhui University of Traditional Medicine;Hefei;Anhui 230031 |
| Abstract: | Aim To analyze and compare different syntheses of capecitabine.Methods Capecitabine was synthesized from 1.2.3-tri-O-acetyl-5-deoxy-D-ribofuranoside and trimethylsilylated 5-fluorocytosine via condensation,acylation and hydrolysis.In the synthesis of 2 ',3'-diacetyl-5'-deoxy-5-fluoro-cytidine,sodium hydroxide was used instead of baking soda to induce the consumption of alkali and the product of salt.Results&Conclusions Proper method was selected by study of temperature and alkali concentration with an overa... |
| Keywords: | ribose cytidine capecitabine synthesis improvement |
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