1,2,4-三唑并[3,4-α]吡啶的最新进展：合成与生物活性,Current Organic Chemistry

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1,2,4-三唑并[3,4-α]吡啶的最新进展：合成与生物活性
Current Organic Chemistry ( IF 1.7 ) Pub Date : 2017-06-30 , DOI: 10.2174/1385272821666170410145554
Zhong-Hua Shen ₁ , Qiao Wang ₁ , Ming-Yan Yang ₁ , Zhao-Hui Sun ₁ , Jian-Quan Weng ₁ , Cheng-Xia Tan ₁ , Hong-Ke Wu ₁ , Liang Han ₁ , Xing-Hai Liu ₂

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背景：含氮杂环是一种最重要的杂环。其中，1,2,4-三唑并[3,4-α]吡啶是经典的五元杂环稠合六元杂环。1,2,4-三唑并-[3,4-α]吡啶骨架已广泛用于药物，农药和其他领域的构件。

方法与目的：本文综述了1,2,4-三唑并[3,4-α]吡啶多样性的合成方法。为了促进更高效，环保的反应的发展，本文详细列出了使用许多缩合剂的合成方法，例如HOAc，原甲酸，Ph3PCl2，Lawesson试剂，PS-PPh3，HCOOH，POCl3，Mitsunobu试剂，Burgess试剂，IBD，金属催化剂，氯胺-T，三价碘试剂等。另外，在微波辐射或常规加热下直接合成1,2,4-三唑并[3,4-α]吡啶。这篇评论还涵盖了针对各种1,2,4-三唑-[3,4-α]吡啶的不同生物活性，包括抗炎活性，抗惊厥活性，抗生素活性，抗真菌活性，

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Recent Advances of 1,2,4-triazolo[3,4-α]pyridines: Synthesis and Bioactivities

Background: Nitrogen containing heterocycle is one kind of the most important heterocycle. Among them, 1,2,4-triazolo[3,4-α]pyridine is a classic five member heterocycle fused six member heterocycle. 1,2,4-Triazolo-[3,4-α ]pyridine scaffold has been widely used in building blocks for drugs, pesticides and other fields.

Method & Objective: This review will highlight the early and recent work on the synthesis methods of diversity 1,2,4-triazolo[3,4-α]pyridines. In order to promote the development of more efficient and environment friendly reaction, this paper detailed that the synthetic procedure has been listed using many condensation agents, such as HOAc, orthoformate, Ph3PCl2, Lawesson reagent, PS-PPh3, HCOOH, POCl3, Mitsunobu reagent, Burgess reagent, IBD, metal catalyst, chloramine-T, trivalent Iodine reagent and so on. Also the 1,2,4- triazolo[3,4-α]pyridines were synthesized under microwave irradiation or conventional heat directly. This review also covers different biological activities towards various 1,2,4-triazolo-[3,4-α]pyridines including antiinflammatory activity, anti-convulsant activity, antibiotics activity, antifungal activity, herbicidal activity, fungicidal activity, anticancer activity, antivirus activity, anti- type 2 diabetes activity, etc.

更新日期：2017-06-30

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