Chemical Industry and Engineering Progree

Previous Articles     Next Articles

Research progresses in chemoenzymatic synthesis of Duloxetine hydrochloride

LI Long1,QIU Guisen2,JIANG Tailong2,ZENG Congming2,YAO Qizheng1   

  1. 1 School of Pharmacy,China Pharmaceutical University,Nanjing 210009 Jiangsu,China;2 Shanghai Amazin Biological Technology Co.,Ltd.,Shanghai 201203,China
  • Online:2014-07-25 Published:2014-07-05

化学酶法合成盐酸度洛西汀的研究进展

李龙1,邱贵森2,蒋泰龙2,曾聪明2,姚其正1   

  1. 1中国药科大学药学院,江苏 南京 210009;2上海艾美晶生物科技有限公司,上海 201203

Abstract: The incidence of depression showed a clear upward trend in the global. Duloxetine is the better antidepressant drugs,there are some disadvantages on the industry for the full chemical synthesis. Enzyme catalysis has mild reaction condition,environmental friendly and synthetic chiral compounds with high enantioselectivity. Introduction of enzymatic can make up for the chemical synthesis. A review of the progress made in this article,we focused on the enzymatic resolution and bio-catalytic asymmetric synthesis critical enantiomer:1-(tetrahydrothioph-en-2-yl)propan-1-ol derivatives. Meanwhile we summarized their advantages and disadvantages and saw the rosy application prospect. Point out that screening high catalytic and high stability of microorganisms is the main direction of enzymatic technology to achieve industrial application.

Key words: Duloxetine hydrochloride, bio-catalysis, enzyme resolution, asymmetry synthesis with biocatalysis

摘要: 抑郁症的发病率在全球呈现明显上升趋势。盐酸度洛西汀是较好的抗抑郁药物,目前工业上采用全化学合成方法存在着一定的缺陷,而酶催化反应条件温和、环境友好,尤其对手性化合物的合成有极高的对映选择性,引入酶法能弥补化学合成的不足。本文针对化学法和酶法相结合制备手性药物盐酸度洛西汀的研究进展进行了综述,重点介绍了酶法拆分和生物催化不对称合成技术制备盐酸度洛西汀关键单一对映中间体:(S)-1-(噻 吩-2-基)-1-仲醇衍生物的策略,分析了它们的优缺点,展望了发展前景,指出筛选高催化性能和高稳定性的微生物是实现酶催化技术工业化应用的主要方向。

关键词: 盐酸度洛西汀, 生物催化, 酶法拆分, 生物催化不对称合成