| 卡培他宾的合成工艺研究 |
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| 引用本文： | 刘杨,骆伟,孙厉,陶然,郭春. 卡培他宾的合成工艺研究[J]. 中国药物化学杂志, 2009, 19(2): 120-122 |
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| 作者姓名： | 刘杨 骆伟 孙厉 陶然 郭春 |
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| 作者单位： | （沈阳药科大学 制药工程学院，辽宁 沈阳 110016） |
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| 摘 要： | 目的 合成抗肿瘤药卡培他宾。方法 以D-核糖为起始原料，通过缩醛保护、对甲苯磺酰化、溴代、氢化脱卤、脱保护和乙酰化共6步反应制得中间体5-去氧-1,2,3-三-O-乙酰基-D-核糖(7)，N4-正戊氧羰基-5-氟胞嘧啶与中间体7进行缩合后，再经氨解脱乙酰基得到目标化合物。结果与讨论 目标化合物的总收率为16.4 %(以D-核糖计)，其结构经1H-NMR、MS确证。该合成工艺简化了操作，降低了合成成本，适于工业化生产。
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| 关 键 词： | 卡培他宾；合成工艺；抗癌 |
| 收稿时间： | 2008-08-28 |
| 修稿时间： | 2009-01-20 |
Study on the synthetic technology of capecitabine |
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| LIU Yang,LUO Wei,SUN Li,TAO Ran,GUO Chun. Study on the synthetic technology of capecitabine[J]. Chinese Journal of Medicinal Chemistry, 2009, 19(2): 120-122 |
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| Authors: | LIU Yang LUO Wei SUN Li TAO Ran GUO Chun |
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| Affiliation: | (School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China) |
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| Abstract: |  Aim To synthesize anticancer agent capecitabine. Methods 5-Deoxy-1,2,3-tri-O-acetyl-D-ri- bofuranoside (7) was prepared from D-ribofuranoside through 6 steps like protection, sulfonylation, bromation, reduction, deprotection and acetylation. Then compound 7 was condensed with 5-fluoro-N4-(pentyloxycarbonyl) cytosine and capecitabine was obtained followed by deprotection . Results and conclusionThe structure of capecitabine was confirmed by 1H-NMR spectrum and MS. The total yield of the process is 16.4 % (based on D-ribofuranoside). This synthetic process is applicable in industrial preparation with a lower cost and simplified operation. |
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| Keywords: | capecitabine synthetic technology anticancer |
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