Green synthesis and antifungal activities of novel 3‐(trifluoromethyl)‐4,5‐dihydro‐1H‐furo[2,3‐c]pyrazole derivatives,Journal of Heterocyclic Chemistry

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Green synthesis and antifungal activities of novel 3‐(trifluoromethyl)‐4,5‐dihydro‐1H‐furo[2,3‐c]pyrazole derivatives
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-05-04 , DOI: 10.1002/jhet.3998
Fangshun Tan ₁ , Shennan Su ₂ , Zhenzhong Liu ₂

Affiliation

Trifluoromethylated molecules, as well as pyrazol‐3‐one derivatives, are found in a wide range of biologically active compounds. An highly facile, green and mild access to substituted 3‐(trifluoromethyl)‐4,5‐dihydro‐1H ‐furo[2,3‐c ]pyrazole derivatives by the cascade [3 + 2] Michael/Alkylation of unsaturated pyrazolones with α‐bromomalonate has been developed. The reactions can be performed in a easily available and environmentally benign solvent, and the substituted 3‐(trifluoromethyl)‐4,5‐dihydro‐1H ‐furo[2,3‐c ]pyrazole derivatives can be obtained in good to excellent yields by a simple purification step. The antifungal activities of these functional pyrazole derivatives were also evaluated and they showed high antifungal activity against Alternaria solani .

中文翻译：

新型3-（三氟甲基）-4,5-二氢-1H-呋喃[2,3-c]吡唑衍生物的绿色合成和抗真菌活性

三氟甲基化分子以及吡唑-3-酮衍生物存在于多种生物活性化合物中。通过不饱和吡唑酮与[3 + 2]的迈克尔/烷基化反应，可轻松，绿色且温和地获得取代的3-（三氟甲基）-4,5-二氢-1 H-呋喃[2,3- c ]吡唑衍生物已经开发了α-溴丙二酸酯。反应可以在容易获得且对环境无害的溶剂中进行，并且取代的3-（三氟甲基）-4,5-二氢-1 H-呋喃[2,3- c通过简单的纯化步骤可以良好的产率获得对吡唑衍生物。这些功能的吡唑衍生物的抗真菌活性也进行了评估，并且对链格孢菌（Alternaria solani）具有很高的抗真菌活性。

更新日期：2020-05-04

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