| 氯法拉滨的合成工艺改进 |
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| 引用本文： | 郭舜民,邓思珊,齐一萍,林绥. 氯法拉滨的合成工艺改进[J]. 中国现代应用药学, 2009, 26(2): 123-125 |
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| 作者姓名： | 郭舜民 邓思珊 齐一萍 林绥 |
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| 作者单位： | 福建省医学科学研究所药物化学室，福州 350001 |
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| 摘 要： | 目的合成标题化合物，并进行工艺改进。方法以1-乙酰基-2，3，5三-O-苯甲酰基-β-D-呋喃核糖为起始原料，制得1-氯-2-脱氧-2-氟-3，5-二-O-苯甲酰基-α—D-阿拉伯糖（化合物6）。化合物6与2-氯腺嘌呤在四氯化锡作用下发生缩合反应生成氯法拉滨。结果总收率为8．4％，目标化合物的结构经IR、^1H—NMR、MS等方法确证。结论该合成工艺具有原料易得，操作简便，易于工业化生产等特点。
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| 关 键 词： | 工艺改进 化学合成 氯法拉滨 抗白血病 |
| 收稿时间： | 1900-01-01 |
Improved Synthesis of Clofarabine |
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| GUO Shunmin,DENG Sishan,QI Yiping,LIN Sui. Improved Synthesis of Clofarabine[J]. The Chinese Journal of Modern Applied Pharmacy, 2009, 26(2): 123-125 |
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| Authors: | GUO Shunmin DENG Sishan QI Yiping LIN Sui |
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| Affiliation: | ( Fufian Institute of Medical Science,Fuzhou 350001, China) |
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| Abstract: | OBJECTIVE To synthesize the title compound and improve the process. METHODS 3,5-di-O-benzoyl-2-deoxy-2- fluoro-α-D-arabinofuranosyl chloride （ compound 6） was synthesizes from 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose. clofarabine was obtained by the reaction of the compound 6 and 2-chloroadenine in the presence of SnC14. RESULTS The total yield was up to 8.4%. The target compound was identified by IR, ^1H-NMR and MS. CONCLUSION The improved process is simple and easy for a scale production. |
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| Keywords: | process improvement chemical synthesis clofarabine antileukemie |
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