应用化学 ›› 2020, Vol. 37 ›› Issue (11): 1236-1248.DOI: 10.11944/j.issn.1000-0518.2020.11.200151

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(R)-α-硫辛酸合成方法的研究进展

韩修a, 康传清b*   

  1. a四川大学化学学院 成都 610064;
    b中国科学院长春应用化学研究所,高分子复合材料工程实验室 长春 130022
  • 收稿日期:2020-05-19 修回日期:2020-06-28 接受日期:2020-07-23 出版日期:2020-11-01 发布日期:2020-11-04
  • 通讯作者: 康传清,研究员; Tel:0431-85262291; E-mail:kangcq@ciac.ac.cn; 研究方向:不对称合成、功能有机分子合成、自组装和生物活性

Advances in Synthetic Methods of (R)-α-Lipoic Acid

HAN Xiua, KANG Chuanqingb*   

  1. aCollege of Chemistry,Sichuan University,Chengdu 610000,China;
    bChangchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun 130022,China
  • Received:2020-05-19 Revised:2020-06-28 Accepted:2020-07-23 Published:2020-11-01 Online:2020-11-04
  • Contact: KANG Chuanqing, professor; Tel:0431-85262291; E-mail:kangcq@ciac.ac.cn; Research interests:asymmetric synthesis, synthesis, self-assembly, and bioactivity of functional organic molecules

摘要: (R)-α-硫辛酸可用于预防和治疗糖尿病及相关并发症,也可以作为保健品使用,用途广泛,因而其高效合成方法长期以来受到广泛关注。 目前,合成(R)-α-硫辛酸的方法主要有酶和化学方法催化的不对称合成、消旋体的手性拆分以及手性底物控制的不对称合成。 本文将以此为分类标准,对目前所报道的(R)-α-硫辛酸合成方法进行总结归纳和展望。

关键词: 硫辛酸, 手性拆分, 不对称合成

Abstract: The methods for the effective synthesis of (R)-α-lipoic acid have been widely investigated since (R)-α-lipoic acid can be widely used for the treatment of diabetes and diabetic complications. It is also extensively used in health care products. Therefore, asymmetric synthesis of (R)-α-lipoic acid has attracted broad interests from the community of both academia and industry. To date, the reported routes for the synthesis of (R)-α-lipoic acid include asymmetric synthesis catalyzed by the enzymatic and chemical catalysts, chiral resolution, and chiral substrate-controlled synthesis. Based on this classification, this paper summarizes the advances of the methods for asymmetric synthesis of (R)-α-lipoic acid and predicts future prospects.

Key words: lipoic acids, chiral resolution, asymmetric synthesis

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