Published as part of the Special Topic Modern Strategies for Heterocycles Synthesis

Abstract

(E)-5-[1-(4-Phenyl-2-oxo-1-oxaspiro[4.5]dec-3-en-3-yl)eth­yl­idene]-2-aminoimidazolin-4-one derivatives, as novel fungicidal agents, are designed and synthesized in moderate to excellent yields in four steps from (1-hydroxycyclohexyl)(phenyl)methanone and diketene as the starting materials. The products are characterized by ¹H NMR and HRMS (ESI) analysis. An in vivo bioassay shows that some of the products exhibit good to excellent inhibition against P. cubensis and C. lagenarium, whilst up to 94.7% inhibition against P. capsici and up to 78.1% inhibition against B. cinerea is demonstrated in the in vitro bioassay. EC₅₀ values of 3.40 and 5.86 μg/mL are demonstrated against P. capsici and B. cinerea.

(E)-5-[1-(4-Phenyl-2-oxo-1-oxaspiro[4.5]dec-3-en-3-yl)eth­yl­idene]-2-aminoimidazolin-4-one derivatives, as novel fungicidal agents, are designed and synthesized in moderate to excellent yields in four steps from (1-hydroxycyclohexyl)(phenyl)methanone and diketene as the starting materials. The products are characterized by ¹H NMR and HRMS (ESI) analysis. An in vivo bioassay shows that some of the products exhibit good to excellent inhibition against P. cubensis and C. lagenarium, whilst up to 94.7% inhibition against P. capsici and up to 78.1% inhibition against B. cinerea is demonstrated in the in vitro bioassay. EC₅₀ values of 3.40 and 5.86 μg/mL are demonstrated against P. capsici and B. cinerea.

中文翻译：

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（E）-5- [1-（4-苯基-2-氧-2-氧-1-氧杂螺[4.5]癸-3-烯-3-基）亚乙基] -2-氨基咪唑啉-4-酮衍生物的合成和杀真菌活性

作为“杂环合成的现代策略”专题的一部分发布

抽象的

（E）-5- [1-（4-苯基-2-氧-1-氧杂螺[4.5] dec-3-en-3-基）亚乙基] -2-氨基咪唑啉-4-酮衍生物，作为新型杀真菌剂以（1-羟基环己基）（苯基）甲酮和双烯酮为起始原料，分四个步骤以中等至极好的收率设计和合成。产物通过¹ H NMR和HRMS（ESI）分析进行表征。的体内生物测定表明，一些产品表现出良好的对抗抑制优良黄瓜霜霉病和黄瓜炭疽病，而高达94.7％的抑制对辣椒疫霉和针对高达78.1％的抑制灰霉病证明在体外生物测定。欧共体针对辣椒辣椒和灰葡萄孢的_50个值分别为3.40和5.86μg/ mL 。

（E）-5- [1-（4-苯基-2-氧-1-氧杂螺[4.5] dec-3-en-3-基）亚乙基] -2-氨基咪唑啉-4-酮衍生物，作为新型杀真菌剂以（1-羟基环己基）（苯基）甲酮和双烯酮为起始原料，分四个步骤以中等至极好的收率设计和合成。产物通过¹ H NMR和HRMS（ESI）分析进行表征。的体内生物测定表明，一些产品表现出良好的对抗抑制优良黄瓜霜霉病和黄瓜炭疽病，而高达94.7％的抑制对辣椒疫霉和针对高达78.1％的抑制灰霉病证明在体外生物测定。欧共体针对辣椒辣椒和灰葡萄孢的_50个值分别为3.40和5.86μg/ mL 。