摘要
背景:杂环化合物是现代药物发现研究的有趣组成部分。按照绿色技术生态友好地合成杂环是保护大自然的特权路线。化学化合物的微波辅助合成被认为是学术界和工业界的主要绿色途径。 方法:回顾总共106篇文献(包括一些真实的网络链接),主要讨论(一)微波辐射机理,(二)商业杂环药物丰富,(三)各种合成程序,(四)医药合成分子的活性。 结果:综述了近年来微波辐射(电介质加热)合成具有重要生物学意义的杂环小分子的潜在应用。大量杂环化合物存在于植物,海洋微生物或其他生物体等各种天然来源中,其中许多具有独特的生物活性。除了天然来源的杂环化合物之外,大量的合成杂环化合物也被用作药物。该综述描述了微波辐射的相关最近实例,以实现由各种催化剂加速的各种化学转化,所述催化剂包括但不限于路易斯酸,其它含金属的催化剂,有机催化剂,非均相催化剂,相转移催化剂,固载催化剂,无机催化剂(碱,酸和盐)等。尽管关于介电加热在各个领域的应用报道越来越多,本文综述了大量与合成有机化学有关的新颖策略。讨论主要由疾病类型组织,尽管一些反应/分子当然可以放在多个部分。由于绿色化学是一个极其新兴和相对较新的研究领域,因此试图刺激更多的绿色药物化学活动。还讨论了微波,催化剂和/或溶剂的共同作用,支持构成药用重要杂环化合物和药效团合成的快速和一般途径。 结论:介电加热法制备新型医学杂环支架/化合物是非常有前景和挑战性的。因此,这种绿色技术越来越受到制药界的关注。最近更新已经提出。尽管已经尽一切努力包括这方面的所有相关报告,但任何疏忽都是无意的。
关键词: 微波,杂环,抗癌,抗菌,抗菌,天然产物,药效团,催化剂。
Current Medicinal Chemistry
Title:Synthesis of Medicinally Privileged Heterocycles through Dielectric Heating
Volume: 24 Issue: 41
关键词: 微波,杂环,抗癌,抗菌,抗菌,天然产物,药效团,催化剂。
摘要: Background: Heterocyclic compounds are intriguing part of modern drug discovery research. Ecofriendly syntheses of heterocycles, following green techniques, are privileged routes to protect Mother nature. Microwave-assisted synthesis of chemical compounds is considered as a major greener pathway, both in academia and industry.
Methods: A total of 106 publications (including a few authentic web links) have been reviewed mainly to discuss (i) mechanism of microwave irradiation, (ii) abundance of commercial heterocyclic drugs, (iii) various synthetic procedures, and (iv) medicinal activity of the synthesized molecules.
Results: This review summarizes the potential application of microwave irradiation (dielectric heating) to synthesize biologically important heterocyclic small molecules in the recent past. A huge number of heterocyclic compounds are present in various natural sources like plant, marine microbe or other organisms and many of them possess unique biological activity. In addition to nature-derived heterocyclic compounds, a large number of synthetic heterocycles are being used as medicines. This review describes the relevant recent examples of microwave irradiation to accomplish various chemical transformations accelerated by a variety of catalysts which include, but not limited to, Lewis acids, other metal containing catalysts, organocatalysts, heterogeneous catalysts, phase-transfer catalysts, solid-supported catalysts, inorganic catalysts (bases, acids and salts) and so on. Although there are an increasing number of reports on application of dielectric heating in various other fields, this review is focused on a large number of new and novel strategies related to synthetic organic chemistry. The discussion is mostly organized by the disease type although some reactions/molecules can certainly be placed in multiple sections. Since green chemistry is an extremely emerging and comparatively new field of research, attempts to stimulate more activities on green medicinal chemistry are provided. Discussion related to the concurrent effect of microwaves, catalysts and/or solvents, supports to constitute expeditious and general route for the syntheses of medicinally important heterocyclic compounds and pharmacophores has also been included.
Conclusion: The dielectric heating procedure to produce novel medicinally privileged heterocyclic scaffolds/ compounds is extremely promising and challenging. As a result, this green technique has been gaining increasing interest from the pharmaceutical world. A recent update has been presented. While every effort has been made to include all pertinent reports in this field, any omission is unintentional.
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Cite this article as:
Synthesis of Medicinally Privileged Heterocycles through Dielectric Heating, Current Medicinal Chemistry 2017; 24 (41) . https://dx.doi.org/10.2174/0929867324666170223152137
DOI https://dx.doi.org/10.2174/0929867324666170223152137 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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