艾地苯醌的简便合成

借鉴Hammamura等提出的醌与环戊二烯进行Diels-Alder反应后, 可将醌羰基α-非酸性的烯氢原子转化为羰基α-氢的原理, 将辅酶Q0(5)与环戊二烯的Diels-Alder反应产物(6)在叔丁醇钾-THF体系中, 与以1,10-癸二醇(1)为原料制成的衍生物(4)进行缩合, 再经逆Diels-Alder反应, 得到艾地苯醌, 该方法步骤简洁、条件温和、重现性好、收率较高.

Simple Synthesis of Idebenone

Idebenone is a synthetic analog of coenzyme Q10.It has clinical applications in many central ner-vous system degenerative diseases associated with oxidative stress,such as Parkinson's and Alzheimer's diseases,and especially in the therapy of Friedreich's ataxia.According to the established method of synthesizing the quinone using 3,4-cyclopendadiene as auxiliary reagent by Hamamura,the target compound with a good productivity was obtained firstly by using the alkylation reaction of quinone as the key step and coenzyme Q0 and 1,10-decanediol as the first materials of main body and side chain,respectively,the reactions proceed smoothly under mild conditions to give the expected proucts in good yields.Contrast to the original method,this method is more simple,efficient and practical.