| 酵母菌DM10不对称合成(R)-(-)邻氯扁桃酸甲酯 |
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| 引用本文： | 田冬梅,马小双,贾 娴,尹 璐,徐慰倬,游 松. 酵母菌DM10不对称合成(R)-(-)邻氯扁桃酸甲酯[J]. 沈阳药科大学学报, 2011, 28(1): 69-72 |
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| 作者姓名： | 田冬梅 马小双 贾 娴 尹 璐 徐慰倬 游 松 |
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| 作者单位： | 1. 沈阳药科大学 生命科学与生物制药学院，辽宁 沈阳110016；2. 沈阳药科大学 制药工程学院，辽宁 沈阳110016 |
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| 基金项目： | 国家自然科学基金项目(20472116) |
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| 摘 要： | 目的合成(S)-氯吡咯雷的关键中间体——(R)-(-)邻氯扁桃酸甲酯,并建立了优化的还原条件。方法以邻氯苯乙酮酸甲酯为底物,利用酵母菌DM10的醇脱氢酶及其辅酶合成(R)-(-)邻氯扁桃酸甲酯,并考察了底物质量浓度、初始pH、转化温度和反应时间对不对称还原的影响。结果和结论获得优化的还原条件:接种量体积分数为10%,初始pH值为6.5,底物质量浓度为1 g.L-1,温度为30℃,转化36 h,转化率为98.75%,产率为82.25%,对映体过量值为95.1%。
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| 关 键 词： | 生物催化 不对称还原 (R)-(-)邻氯扁桃酸甲酯 酵母菌DM10 |
| 收稿时间： | 2010-03-10 |
| 修稿时间： | 2010-05-10 |
Asymmetric synthesis of methyl (R)-o-chloromandelate by Saccharomyces cerevisiae DM10 |
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| TIAN Dong-mei,MA Xiao-shuang,JIA Xian,YIN Lu,XU Wei-zhuo,YOU Song. Asymmetric synthesis of methyl (R)-o-chloromandelate by Saccharomyces cerevisiae DM10[J]. Journal of Shenyang Pharmaceutical University, 2011, 28(1): 69-72 |
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| Authors: | TIAN Dong-mei MA Xiao-shuang JIA Xian YIN Lu XU Wei-zhuo YOU Song |
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| Affiliation: | 1(1.School of Life Science and Biopharmaceutics,Shenyang Pharmaceutical University,Shenyang 110016,China;2.School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China) |
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| Abstract: | Objective To prepare methyl (R)-o-chloromandelate (key intermediate for (S)-clopidogrel ) and establish the optimal conditions. Methods Methyl 2-chlorobenzoylformate was transformed to methyl (R)-o-chloromandelate by enzyme system of alcohol dehydrogenase and coenzyme in Saccharomyces cerevisiae DM10. Effects of some factors on the asymmetric reduction, including substrate concentrations, initial pH, temperature and reaction time, were studied. Results and conclusion The optimal reaction conditions was obtained:10% inoculums of the conversion solution, substrate concentration was 1 g·L-1,the initial pH value was 6.5,temperature was set at 30 °C,the reaction was maintained for 36 h,the conversion was 98.75% with the yield of 82.25% and enantiomeric excess of 95.1%. |
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| Keywords: | biocatalysis asymmetric reduction methyl(R)-o-chloromandelate Saccharomyces cerevisiae DM10 |
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