| 地尔硫卓手性中间体合成进展 |
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| 引用本文： | 潘江,许建和,叶勤.地尔硫卓手性中间体合成进展[J].生物加工过程,2009,7(3):9-15. |
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| 作者姓名： | 潘江 许建和 叶勤 |
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| 作者单位： | 华东理工大学,生物反应器工程国家重点实验室,上海,200237 |
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| 基金项目： | 国家高技术研究发展计划(863计划) |
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| 摘 要： | 地尔硫卓是重要的心血管药物，在其分子结构中含有2个手性中心，可产生4个立体异构体，其中只有（2s，3s）-异构体具有药理活性，因此其立体选择性合成具有很大的挑战性。研究人员采用多种方法合成单一构型的地尔硫卓手性中间体，其中包括化学拆分、化学不对称合成以及化学-酶法合成等方法。对地尔硫卓手性中间体的制备方法进行了综述。
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| 关 键 词： | 地尔硫卓 手性中间体 拆分 不对称合成 化学-酶法合成 |
Advance in synthesis of chiral intermediate for diltiazem |
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| PAN Jiang,XU Jian-he,YE Qin.Advance in synthesis of chiral intermediate for diltiazem[J].Chinese Journal of Bioprocess Engineering,2009,7(3):9-15. |
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| Authors: | PAN Jiang XU Jian-he YE Qin |
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| Institution: | (State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, China) |
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| Abstract: | Diltiazem is an important coronary vasodilating drug and contains two chiral centers while only the （2S, 3S）-isomer has the desired activity. Many methods were investigated for the synthesis of the single enantiomer of the chiral intermediate, including chemical resolution, chemical asymmetric synthesis and chemo-enzymatie synthesis. In this paper, these methods for the preparation of diltiazem intermediate were reviewed. |
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| Keywords: | diltiazem chiral intermediate resolution asymmetric synthesis chemo-enzymatic synthesis |
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