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本文以香草醛、藜芦醛及胡椒醛的肟化合物(Ⅳ,Ⅴ,Ⅵ)与α-取代的脂肪酰卤,取代苯甲酰氯和芳杂环取代的甲酰氯反应合成了三类相应的肟酯衍生物,计二十六个(Ⅶa～f,Ⅷa～j,Ⅸa～j)。在二环己基碳二亚胺存在下,用苯乙酸酰化得胡椒醛肟(Ⅵ),E-型的(Ⅵa)可形成胡椒醛肟苯乙酸酯(Ⅸh),而Z-型的(Ⅵb)脱水转比为腈。本文还对部分化合物进行了初步的药理试验,藜芦醛肟呋喃甲酸酯(Ⅷa)和胡椒醛肟噻吩甲酸酯(Ⅸb)有抗电休克惊厥活性,且毒性较小。
In this paper, the oxime compounds (Ⅳ, Ⅴ, Ⅵ) of vanillin, veratraldehyde and piperonal were reacted with α-substituted fatty acyl halides, substituted benzoyl chlorides and aromatic heterocyclic substituted carbonyl chlorides to synthesize three kinds of corresponding oximes Twenty-six (VIIa ~ f, Ⅷa ~ j, Ⅸa ~ j). Acrylated with phenylacetic acid in the presence of dicyclohexylcarbodiimide to afford piperdone oxime (VI), E-type (VIa) forms piperdone oxime phenylacetate (IXh) and the Z- Ⅵb) The dehydration conversion is nitrile. In this paper, some of the compounds were also preliminary pharmacological tests, veratridoxime furoate (Ⅷ a) and piperdoline oxime thiophenecarboxylate (Ⅸ b) have anticonvulsant convulsion activity, and less toxic.