Department of Chemistry, K.J. Somaiya College, Kopargaon-423601, Maharashtra, India.
Department of Chemistry, Maharashtra Udayagiri College, Udgir-413517, Maharashtra, India.
Curr Org Synth. 2022 Aug 6;19(6):693-701. doi: 10.2174/1570179419666220304160938.
The aim of this present work was to design and establish an efficient synthesis of new thienyl pyrazolo[1,5-a] pyrimidines using an environmentally friendly reaction solvent. Further, the newly synthesized compounds were evaluated for antimicrobial activity.
A series of thienyl pyrazolo[1,5-a] pyrimidines have been synthesized by the condensation reaction of 4-(4'-chloro-phenylazo)-5-amino pyrazole with α, β- unsaturated carbonyl composites (chalcones) using NaOH in polyethylene glycol- 400 as a green reaction solvent. The dissemination technique recommended by the National Clinical Laboratory Standards Committee was used to study the antimicrobial activities of synthesized compounds.
Polyethylene glycol-400 prompting an efficient synthesis of thienyl pyrazolo[1,5-a] pyrimidines have been discussed. Excellent yields of the products were obtained in a shorter reaction time using PEG 400 as a green reaction solvent. The reaction solvent was recovered and reused without the loss of its activity. The synthesized compounds have shown interesting antibacterial activity. Hydroxyl and halo substitution with thienyl moiety emerged as an active antibacterial and antifungal study.
The advantage of this methodology is that it incorporates the green method, has excellent yields, easy workup, avoids toxic solvents, and an expensive catalyst. The new dimension pyrazolo[1,5-a] pyrimidine derivatives with thienyl moiety exhibit promising anti-microbial activity.
本研究旨在设计并建立一种使用环保反应溶剂高效合成新型噻吩并吡唑并[1,5-a]嘧啶的方法。此外，还评估了新合成的化合物的抗菌活性。
通过 4-(4'-氯苯基偶氮)-5-氨基吡唑与α,β-不饱和羰基化合物（查耳酮）在聚乙二醇-400 中用 NaOH 缩合反应，合成了一系列噻吩并吡唑并[1,5-a]嘧啶。采用美国国家临床实验室标准委员会推荐的扩散技术研究了合成化合物的抗菌活性。
讨论了聚乙二醇-400 促进噻吩并吡唑并[1,5-a]嘧啶高效合成的情况。使用 PEG 400 作为绿色反应溶剂，可以在更短的反应时间内获得优异的产率。反应溶剂可以回收并重复使用，而不会失去其活性。合成的化合物表现出有趣的抗菌活性。噻吩取代基上的羟基和卤代取代基表现出良好的抗菌和抗真菌活性。
该方法的优点是采用了绿色方法，产率高，操作简单，避免了使用有毒溶剂和昂贵的催化剂。噻吩取代基的新型吡唑并[1,5-a]嘧啶衍生物具有良好的抗菌活性。
