糖尿病综合症新药Epalrestat的光敏异构化研究

Study of New Remedy for Diabetes Sympatomatology Epalrestat's Light Sensitive Isomerization

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。

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 a - 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.