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芳环邻位取代的Z、E型-α-卤代桂皮酰胺类化合物的合成与抗惊活性的研究
SYNTHESIS AND ANTICONVULSANT-ACTIVITY IN (Z), (E)-ORTHO-SUBSTITUTED-α-HALOCINNAMAMIDES
【摘要】 通过苯环邻位取代的α,β-二氯苯丙酸的碱性消除反应可制得Z.E型-α-氯代桂皮酸,再经酰氯化及胺解可分别得到α-氯代桂皮酰胺的Z型及E型异构体。药理实验表明,邻位取代的α-氯代桂皮酰胺中E型体的抗惊作用强于Z型异构体。
【Abstract】 The (Z), (E)-α-chlorocinnamic acid can be acquired by the alkaline elimination of ortho-subs-tituted-α,β-dichlorophenylpropionic acid. The substituted cinnamic acids were converted into corres-ponding (Z), (E)-O-substituted-α-chlorocinnamamides by means of acid chlorides. The pharmacolo-gical evaluation showed that the configuration of amides displayed important effect. The anticonvul-sant activity of (E)-geometrical isomers are stronger than (Z)-isomers.
【关键词】 邻位取代的-α-卤代桂皮酰胺;
抗惊活性;
几何异构体;
构型;
【基金】 国家自然科学基金
- 【文献出处】 北京医科大学学报 , 编辑部邮箱 ,1988年04期
- 【被引频次】1
- 【下载频次】52