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具有预期生物活性的4(H)-1,2,4-三唑衍生物。第四部分。取代的3,4,5-三芳基-1,2,4-三唑的合成。

4(H)-1,2,4-triazole derivatives with expected biological activity. Part IV. Synthesis of substituted 3,4,5-triaryl-1,2,4-triazoles.

作者信息

Lange J, Tondys H

出版信息

Pol J Pharmacol Pharm. 1975 Apr-Jun;27(2):211-6.

PMID:1153353
Abstract

A series of 23 3,4,5-triaryl-1,2,4-triazoles with various substituents in one, two, or all three aromatic rings were prepared for screening tests as potential antibacterial, mostly antituberculotic agents. The synthesis, depending on the nature and position of the substituents, was accomplished by one of the following methods; (A) condensation of symmetrically substituted bis(alpha-chlorobenzylidene)hydrazine with an aniline derivative; (B) reaction of an aniline derivative with a symmetrical diaroylhydrazine in the presence of PCL3; (C) direct condensation of aroylhydrazine with an appropriately substituted N-phenylbenzimidoyl chloride. The latter method was considered to be most advantageous; it warranted highest yield and purity of the products and made it possible to prepare triazoles with three different aryl groups.

摘要

制备了一系列23种在一个、两个或所有三个芳环上带有各种取代基的3,4,5-三芳基-1,2,4-三唑,用于作为潜在的抗菌剂,主要是抗结核剂的筛选试验。根据取代基的性质和位置,合成通过以下方法之一完成:(A) 对称取代的双(α-氯亚苄基)肼与苯胺衍生物缩合;(B) 苯胺衍生物与对称二芳酰肼在三氯化磷存在下反应;(C) 芳酰肼与适当取代的N-苯基苯甲酰氯直接缩合。后一种方法被认为是最有利的;它保证了产品的最高产率和纯度,并使得制备具有三个不同芳基的三唑成为可能。

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