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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Microwave enhanced solid support synthesis of fluorine containing benzopyrano-triazolo-thiadiazepines as potent anti-fungal agents.
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Microwave enhanced solid support synthesis of fluorine containing benzopyrano-triazolo-thiadiazepines as potent anti-fungal agents.

机译:微波增强的固体支持物合成的含氟苯并吡喃基-三唑并噻二氮杂卓类化合物为有效的抗真菌剂。

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摘要

A facile, dry media procedure has been developed for the synthesis of a series of a new class of fluorine containing 3-alkyl-7-chloro-11a,12-dihydro-11-phenyl-12-(substituted aryl)-11H-benzopyrano[4,3-e][1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazepines (4a-k) under microwaves using basic alumina as solid support. The reaction time has been brought down from hours (60-65 h) to minutes (3-5 min) with improved yield as compared to conventional method, demonstrating the versatility of the process. The method reported herein is devoid of the hazards of solution-phase reactions. The synthesized compounds have been screened 'in vitro' for anti-fungal activity against Rhizoctonia solani, Fusarium oxysporum and Collectotrichum capsici. Most of the compounds have shown good activity against these pathogens.
机译:已经开发了一种简便的干燥介质方法,用于合成一系列新型的含氟的3-烷基-7-氯-11a,12-二氢-11-苯基-12-(取代的芳基)-11H-苯并吡喃基氟在使用碱性氧化铝作为固体载体的微波作用下,[4,3-e] [1,2,4]-三唑并[3,4-b] [1,3,4]-噻二氮卓(4a-k)。与传统方法相比,反应时间从数小时(60-65小时)缩短至数分钟(3-5分钟),并提高了产率,证明了该方法的多功能性。本文报道的方法没有溶液相反应的危害。已对“合成化合物”进行了“体外”筛选,以检测其对茄状根瘤菌,尖孢镰刀菌和辣椒辣椒的抗真菌活性。大多数化合物已显示出对这些病原体的良好活性。

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