Bandyopadhyay Debasish, Banik Bimal K
Department of Chemistry, The University of Texas Rio Grande Valley, 1201 West University Drive, Edinburg, Texas 78539, United States.
Community Health Systems of South Texas, 3135 Sugar Road, Edinburg Texas 78539, United States.
Curr Med Chem. 2017;24(41):4596-4626. doi: 10.2174/0929867324666170223152137.
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.
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.
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.
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.
杂环化合物是现代药物发现研究中引人关注的一部分。采用绿色技术对杂环化合物进行环境友好型合成,是保护大自然的优先途径。在学术界和工业界,微波辅助合成化合物都被视为一条主要的更环保途径。
共查阅了106篇出版物(包括一些可靠的网页链接),主要讨论(i)微波辐射的机制,(ii)市售杂环药物的数量,(iii)各种合成方法,以及(iv)合成分子的药用活性。
本综述总结了微波辐射(介电加热)在近期合成具有生物学重要性的杂环小分子方面的潜在应用。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外,大量合成杂环化合物也被用作药物。本综述描述了微波辐射在各种催化剂加速下完成各种化学转化的相关近期实例,这些催化剂包括但不限于路易斯酸、其他含金属催化剂、有机催化剂、多相催化剂、相转移催化剂、固体负载催化剂、无机催化剂(碱、酸和盐)等。尽管关于介电加热在其他各个领域应用的报道越来越多,但本综述聚焦于与合成有机化学相关的大量新策略。讨论大多按疾病类型组织,尽管有些反应/分子肯定可归入多个部分。由于绿色化学是一个极其新兴且相对较新的研究领域,本文尝试激发更多关于绿色药物化学的研究活动。还纳入了与微波、催化剂和/或溶剂的协同效应相关的讨论,这些讨论有助于构建合成具有药用重要性的杂环化合物和药效基团的快速通用途径。
通过介电加热过程生产新型药用优势杂环骨架/化合物极具前景且具有挑战性。因此,这种绿色技术越来越受到制药界的关注。本文给出了近期的进展情况。尽管已尽力纳入该领域的所有相关报道,但如有任何遗漏,纯属无意。