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异恶唑的无金属合成路线概述:优势骨架

An overview of metal-free synthetic routes to isoxazoles: the privileged scaffold.

作者信息

Das Soumyadip, Chanda Kaushik

机构信息

Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology Vellore-632014 India

出版信息

RSC Adv. 2021 Oct 6;11(52):32680-32705. doi: 10.1039/d1ra04624a. eCollection 2021 Oct 4.

Abstract

In the field of drug discovery, isoxazole is a five-membered heterocyclic moiety commonly found in many commercially available drugs. In view of their enormous significance, it is always imperative to unleash new eco-friendly synthetic strategies. Among various novel synthetic techniques in use for isoxazole synthesis, most synthetic methods employ Cu(i) or Ru(ii) as catalysts for (3 + 2) cycloaddition reaction. The particular disadvantages associated with metal-catalyzed reactions are high costs, low abundance, toxicity, a significant generation of waste, and difficulty to separate from the reaction mixtures. In view of these drawbacks, it is always imperative to develop alternate metal-free synthetic routes. This review article highlights a comprehensive overview on the potential application of metal-free synthetic routes for the synthesis of isoxazoles with significant biological interests.

摘要

在药物研发领域,异恶唑是一种常见于许多市售药物中的五元杂环部分。鉴于其重大意义,开发新的环保合成策略始终至关重要。在用于异恶唑合成的各种新型合成技术中,大多数合成方法采用Cu(i)或Ru(ii)作为(3 + 2)环加成反应的催化剂。与金属催化反应相关的特定缺点包括成本高、丰度低、毒性大、产生大量废物以及难以从反应混合物中分离。鉴于这些缺点,开发替代的无金属合成路线始终至关重要。这篇综述文章重点全面概述了具有重要生物学意义的无金属合成路线在异恶唑合成中的潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b41/9042182/fce6f5921f92/d1ra04624a-f1.jpg

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