| 氮杂胞苷的合成工艺研究 |
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| 引用本文： | 郭刚,杨千姣,赵力挥,刘丹,赵临襄.氮杂胞苷的合成工艺研究[J].中国药物化学杂志,2008,18(5):377-378. |
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| 作者姓名： | 郭刚 杨千姣 赵力挥 刘丹 赵临襄 |
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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： | 以氰基胍和甲酸为原料,经成盐、环合反应得到5-氮杂胞嘧啶,5-氮杂胞嘧啶经硅烷化保护后,与乙酰化的核糖成苷,再脱保护基得到氮杂胞苷。目标化合物的结构经1H-NMR、MS谱数据确证,总收率为26.6%。该工艺路线优化了反应条件、简化了操作、提高了收率。
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| 关 键 词： | 工艺改进 化学合成 氮杂胞苷 氰基胍 |
| 收稿时间： | 2008-4-10 |
| 修稿时间： | 2008-7-8 |
Improved synthesis of azacytidine |
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| GUO Gang,YANG Qian-jiao,ZHAO Li-hui,LIU Dan,ZHAO Lin-xiang.Improved synthesis of azacytidine[J].Chinese Journal of Medicinal Chemistry,2008,18(5):377-378. |
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| Authors: | GUO Gang YANG Qian-jiao ZHAO Li-hui LIU Dan ZHAO Lin-xiang |
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| Institution: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University,Shenyang 110016,China |
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| Abstract: | Cyanoguanidine and acetylated β-D-ribose were used as starting materials to give target compound via salt formation, cyclization, silylation, coupling reaction and deprotection. The target compound was characterized by 1H-NMR, MS spectra and the total yield was 26.6%. The synthetic conditions were optimized and the total yield was increased. |
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| Keywords: | process improvement chemical synthesis azacytidine cyanoguanidine |
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