N-(3,5-二甲氧基-4-烷氧基苯乙基)扁桃酰胺类杀菌剂的设计合成及杀菌活性

Synthesis and fungicidal activity of N-(4-alkoxy-3,5- dimethoxyphenethyl)-mandelamide compounds

摘要: 以第一个扁桃酰胺类杀菌剂双炔酰菌胺为模板,在炔丙氧基的邻位引入第二个甲氧基,设计合成了15个未见文献报道的 N-(3,5-二甲氧基-4-烷氧基苯乙基)扁桃酰胺类化合物(8a～8o),其结构通过核磁共振氢谱和高分辨质谱确认。初步的离体和活体杀菌试验结果表明,化合物 8e、8h和8o 对辣椒疫霉 Phytophthora capsici 具有较好的杀菌活性,其中 8h和8o 在62.5 mg/L下对辣椒疫霉活体抑制率达100%。

Abstract: Mandipropamid is the first mandelamide fungicide on the market.Fifteen new compounds(8a-8o) of N-(4-alkoxy-3,5-dimethoxyphenethyl) mandelamide that the second OCH3 were introduced to the aromatic ring of the phenylethylamine moiety of mandipropamid were designed and synthesized using Vanillin as starting material.Their structures were confirmed by 1H NMR and HRMS.The preliminary bioassay showed that some compounds 8e,8h and 8o have good fungicidal activity.The compound 8h and 8o showed 100% inhibition rate at 62.5 mg/L against Phytophthora capsici in vivo.