| 硼氢化立体选择性还原制备拉米夫定的研究 |
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| 引用本文： | 徐伟明,;黄卓豪,;李万梅,;游金宗,;蒋善会,;章鹏飞.硼氢化立体选择性还原制备拉米夫定的研究[J].杭州师范学院学报(自然科学版),2014(4):370-372. |
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| 作者姓名： | 徐伟明 ;黄卓豪 ;李万梅 ;游金宗 ;蒋善会 ;章鹏飞 |
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| 作者单位： | [1]杭州师范大学材料与化学化工学院,浙江杭州310036; [2]浙江外国语学院理工学院,浙江杭州310012; [3]杭州科本药业有限公司,浙江杭州310004 |
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| 基金项目： | 浙江省自然科学基金项目（Y4100077）;浙江省创新团队项目（2010R50017）;杭州市重大科技项目（20122511A43）. |
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| 摘 要： | 在对核苷类抗病毒药物拉米夫定的制备进行文献综述的基础上，提出一条立体选择硼氢化还原的合成路线合成了拉米夫定．反应中形成的六元环过渡态结构有效抑制消旋化，使得反应过程工艺简单，产品纯度好，收率高，完全符合作为原料药的使用要求．
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| 关 键 词： | 拉米夫定 硼氢化 立体选择 还原 六元环过渡态 |
On the Stereo-selective Reduction and Preparation of Lamivudine through Borohydride |
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| Institution: | XU Weiming , HUANG Zhuohao, LI Wanmei , YOU Jinzong, JIANG Shanhui , ZHANG Pengfei (1. College of Material Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036, China2. School of Science and Technology, Zhejiang International Studies University, Hangzhou 310012, China; 3. Hangzhou Cohen Pharmaceutical Co.,I.td., Hangzhou 310004, China) |
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| Abstract: | Basing on the literature about the preparation of nucleoside antiviral drug Lamivudine, the paper provided a stereo-selective synthetic route by borohydride as the reducing agent. The formed six-membered ring transition state structure effectively inhibited the racemization, it made the reaction process have the advantages of simple process, pure product and high yield, which completely accorded with the usage requirements as the crude drug. |
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| Keywords: | Lamivudine borohydride stereo-selectivity reduction six-membered ring transition state |
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