摘要
苯并咪唑支架存在于各种治疗剂中,并已被认为是用于多种生物活性的基本药效团。这些产生了兴趣和必要性来开发这些特殊类别的化合物的有效合成方法以产生用于各种疾病的新的治疗线索。在几篇综述文章中总结了苯并唑的生物活性及其合成的努力。鉴于此,本文综述的目的是为了说明在微波辐射下合成生物相关的吲哚类化合物所发生的事态发展,因为微波加热的应用一直被认为是快速生成合成目标。注意力集中在那些文献报道中,其中微波辐射的使用是形成杂环系统的关键步骤或者是将吲哚环系统官能化以产生基本药效学特征。通过使用微波辐射合成这些特殊类型的杂环的方便和经济的方式将有利于药物发现科学家合成具有生物活性的吲哚并提供广泛的用于合成吲哚的反应构成这个主题评论。已经绘制了实例,其中与常规加热下合成所观察到的相比,使用微波加热在提高产物收率和缩短反应时间方面提供了明显的优势。
关键词: 2-氨基苯硫酚,邻苯二胺,羧酸,醛,苯并恶唑,苯并噻唑,苯并咪唑,双杂环骨架,稠环体系,生物活性,无催化剂反应,无溶剂反应,固体载体,常规加热,微波辐射,多组分反应,一锅反应,多米诺反应,迈克尔反应,绿色化学等。
Current Medicinal Chemistry
Title:Microwave Assisted Synthesis of Biorelevant Benzazoles
Volume: 24 Issue: 41
关键词: 2-氨基苯硫酚,邻苯二胺,羧酸,醛,苯并恶唑,苯并噻唑,苯并咪唑,双杂环骨架,稠环体系,生物活性,无催化剂反应,无溶剂反应,固体载体,常规加热,微波辐射,多组分反应,一锅反应,多米诺反应,迈克尔反应,绿色化学等。
摘要: The benzazole scaffolds are present in various therapeutic agents and have been recognized as the essential pharmacophore for diverse biological activities. These have generated interest and necessity to develop efficient synthetic methods of these privileged classes of compounds to generate new therapeutic leads for various diseases. The biological activities of the benzazoles and efforts towards their synthesis have been summarized in a few review articles. In view of these, the aim of this review is to provide an account of the developments that have taken place in the synthesis of biorelevant benzazoles under microwave irradiation as the application of microwave heating has long been recognized as a green chemistry tool for speedy generation of synthetic targets. Attention has been focused to those literature reports wherein the use of microwave irradiation is the key step in the formation of the heterocyclic ring system or in functionalization of the benzazole ring system to generate the essential pharmacophoric feature. The convenient and economic way to synthesize these privileged class of heterocycles through the use of microwave irradiation that would be beneficial for the drug discovery scientist to synthesize biologically active benzazoles and provide access to wide range of reactions for the synthesis of benzazoles constitute the theme of this review. Examples have been drawn wherein the use of microwave heating offers distinct advantage in terms of improved product yields and reduction of reaction time as compared to those observed for the synthesis under conventional heating.
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Cite this article as:
Microwave Assisted Synthesis of Biorelevant Benzazoles, Current Medicinal Chemistry 2017; 24 (41) . https://dx.doi.org/10.2174/0929867323666161025142005
DOI https://dx.doi.org/10.2174/0929867323666161025142005 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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