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有机化学
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有机化学 ›› 1999, Vol. 19 ›› Issue (2): 153-156. 上一篇    下一篇

研究论文

糖尿病综合症新药Epalrestat的光敏异构化研究

屠惠萍;将咏文;王隽;华正茂;杨俐苹   

  1. 华东师范大学化学系.上海(200062)
  • 发布日期:1999-04-25

Study of new remedy for diabetes sympatomatology Epalrestat's light sensitive isomerization

Tu Huiping;Jiang Yongwen;Wang Juan;Hua Zhengmao;Yang Liping   

  1. E China Normal Univ, Dept Chem.Shanghai(200062)
  • Published:1999-04-25

被引次数

1

Epalrestat是一种治疗糖尿病晚期综合症的新药。它可以缓解糖尿病型视网膜病变,运动神经传导阻滞等症状。绕丹宁乙酸与α-甲基肉桂醛在乙酸中缩合得到了Epalrestat,并利用了高压液相色谱,X衍射,高分辨率核磁共振,对它的立体异构进行了研究,还研究了它的保存条件。发现Epalrestat的四个立体异构体中(Z,E)构型占96.5%。见光后易发生异构化,产物中(Z,Z)构型的含量可达到37.7%。而避光保存一年后(Z,E)仍能保持93.6%的含量。

关键词: 光敏化, 异构化, Ｘ射线衍射分析, 绕丹宁乙酸, 缩合, 噻唑P, 高速液体色谱, 乙酸P, 甲基肉桂醛, 糖尿病

Epalrestat is a new remedy for diabetes sympatomaology. It can relieve diabetic retinopathy, dibetic motor never conduction inhabition. We synthesized it by rhodanine-3-actic acid and α-methyl- cinnamaldehyde. We researched Epalrestat's configurations and its preserved cinditions with HPLC, X-ray diffraction and high resolving NMR. We discovered, in Epalrestat's four stereo configurations, that (Z, E) is the most stable one (96.5%). But it is easy to transfer to (Z, Z) configuration in the sun light. (Z, E) configuration still has 93.5% in the mixture in dark after one year.

Key words: ACETIC ACID P, PHOTOSENSITIZATION, X-RAY DIFFRACTION ANALYSIS, HIGH SPEED LIQUID CHROMATOGRAPHY, THIAZOLE P, ISOMERIZATION, CONDENSATION, DIABETES MELLITUS

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