Tetrazoles via Multicomponent Reactions.,Chemical Reviews

当前位置： X-MOL 学术 › Chem. Rev. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Tetrazoles via Multicomponent Reactions.
Chemical Reviews ( IF 51.4 ) Pub Date : 2019-02-01 , DOI: 10.1021/acs.chemrev.8b00564
Constantinos G Neochoritis ₁ , Ting Zhao ₁ , Alexander Dömling ₁

Affiliation

Tetrazole derivatives are a prime class of heterocycles, very important to medicinal chemistry and drug design due to not only their bioisosterism to carboxylic acid and amide moieties but also to their metabolic stability and other beneficial physicochemical properties. Although more than 20 FDA-approved drugs contain 1 H- or 2 H-tetrazole substituents, their exact binding mode, structural biology, 3D conformations, and in general their chemical behavior is not fully understood. Importantly, multicomponent reaction (MCR) chemistry offers convergent access to multiple tetrazole scaffolds providing the three important elements of novelty, diversity, and complexity, yet MCR pathways to tetrazoles are far from completely explored. Here, we review the use of multicomponent reactions for the preparation of substituted tetrazole derivatives. We highlight specific applications and general trends holding therein and discuss synthetic approaches and their value by analyzing scope and limitations, and also enlighten their receptor binding mode. Finally, we estimated the prospects of further research in this field.

中文翻译：

通过多组分反应生成四唑。

四唑衍生物是一类主要的杂环化合物，对于药物化学和药物设计非常重要，因为它们不仅具有与羧酸和酰胺部分的生物等排性，而且还具有代谢稳定性和其他有益的理化特性。尽管 FDA 批准的 20 多种药物含有 1 H-或 2 H-四唑取代基，但它们的确切结合模式、结构生物学、3D 构象以及一般化学行为尚未完全了解。重要的是，多组分反应（MCR）化学提供了多种四唑支架的聚合途径，提供了新颖性、多样性和复杂性三个重要元素，但四唑的 MCR 途径还远未完全探索。在这里，我们回顾了多组分反应在制备取代四唑衍生物中的应用。我们重点介绍其中的具体应用和总体趋势，并通过分析范围和局限性讨论合成方法及其价值，并阐明其受体结合模式。最后，我们对该领域的进一步研究前景进行了展望。

更新日期：2019-02-01

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南