α-卤代-间-三氟甲基桂皮酰胺类化合物的合成及其抗惊活性的探讨

The Synthesis and Anticonvulsant Activity of Someα-Halo-m-Trifluoromethyl Cinnamamides

从三氟甲苯始,经溴化、格氏反应、缩合、溴(或氯)加成等反应,合成了九个α-卤代-间-三氟甲基桂皮酰胺和二个α,β-二卤代-间-三氟甲基苯丙酰另丁胺等衍生物。用核磁共振氢谱确定了其Z、E构型。药理结果表明,α-卤素的引入,其抗惊活性未见增强。

Nineα-halo-m-trifluoromethyl cinnamides were synthesized from trjfluoro-methyl benzene,via bromination,Grignard reaction,condensation,halogen addition reactions etc,as indicated in the synthetic scheme.Their configurations were confirmed by NMR.Their pharmacological results showed that,the introduction ofα-halogen group,did not enhance their anticonvulsant activity as expected.