| 抗白血病药氯法拉滨的合成 |
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| 引用本文： | 柴雨柱,牛犇,鲁亚洲,朱先锋,陈严波.抗白血病药氯法拉滨的合成[J].化工时刊,2010,24(8):36-38. |
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| 作者姓名： | 柴雨柱 牛犇 鲁亚洲 朱先锋 陈严波 |
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| 作者单位： | 江苏济川制药有限公司药物研究院,江苏,泰兴,225441 |
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| 摘 要： | 以1-O-乙酰基-2,3,5-三-O-苯甲酰基-β-D-呋喃核糖为起始原料经溴化、重排、酯化、氟代、溴代、缩合、脱保护等反应制得氯法拉滨。所得产物经元素分析、红外光谱、核磁共振谱及质谱等确证结构。此工艺路线方法简便,原料易得,便于工业化生产。
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| 关 键 词： | 氯法拉滨 抗白血病药 合成 |
Synthesis of Antileukemia Drug Clofarabine |
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| Chai Yuzhu,Niu Ben,Lu Yazhou,Zhu Xianfeng,Chen Yanbo.Synthesis of Antileukemia Drug Clofarabine[J].Chemical Industry Times,2010,24(8):36-38. |
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| Authors: | Chai Yuzhu Niu Ben Lu Yazhou Zhu Xianfeng Chen Yanbo |
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| Affiliation: | Chai Yuzhu Niu Ben Lu Yazhou Zhu Xianfeng Chen Yanbo (R＆D Institute of Jumpcan Pharmaceutical Co.Ltd,Jiangsu Taixin 225441) |
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| Abstract: | Objective： To synthesize clofarabine and optimize the process.Methods： Bromination of 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose,followed by a reaction sequence of rearragement,esterification,fluorination,bromination,condensation and deprotection,afforded the title compound.Results： Chemical structure of Clofarabine was confirmed by element analysis,UV,IR,1H-NMR,13C-NMR and ESI-MS etc.Conclusion： This process can be easily controlled and is suitable for a scale production. |
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| Keywords: | clofarabine antileukemia drug synthesis |
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