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Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry

Nitrogen containing heterocycles are of immense research interest because they are often found as naturally occurring bioactive compounds. The prominence of N-heterocycles makes it vital to develop methods to increase their synthetic efficiencies and probe the effects of their modifications on biolo...

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Autores principales: Henary, Maged, Kananda, Carl, Rotolo, Laura, Savino, Brian, Owens, Eric A., Cravotto, Giancarlo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9051880/
https://www.ncbi.nlm.nih.gov/pubmed/35498463
http://dx.doi.org/10.1039/d0ra01378a
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author Henary, Maged
Kananda, Carl
Rotolo, Laura
Savino, Brian
Owens, Eric A.
Cravotto, Giancarlo
author_facet Henary, Maged
Kananda, Carl
Rotolo, Laura
Savino, Brian
Owens, Eric A.
Cravotto, Giancarlo
author_sort Henary, Maged
collection PubMed
description Nitrogen containing heterocycles are of immense research interest because they are often found as naturally occurring bioactive compounds. The prominence of N-heterocycles makes it vital to develop methods to increase their synthetic efficiencies and probe the effects of their modifications on biological efficacy. Medicinal chemists have exploited microwave-assisted organic synthesis (MAOS) to facilitate the development of complex heterocyclic structures. MAOS is a growing synthetic methodology among medicinal chemists and has proven to be more efficient in terms of reaction yield, reaction time, product purity and environmental friendliness for many reactions when compared to conventional thermal methods for cycloaddition and selective functionalization. The importance of nitrogen containing ring systems in medicine cannot be understated, as such ring systems have shown to be applicable in compounds such as vitamins, herbicides, anti-fungal agents, anti-bacterial agents and anti-cancer agents, among other things. The significance of these applications has created an unprecedented need for more efficient synthetic methods. This review presents an overview of MAOS and its role in recent and pressing advancements for the synthesis of small- and medium-sized nitrogen containing heterocycles, including pyrroles, indoles, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with medicinal uses.
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spelling pubmed-90518802022-04-29 Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry Henary, Maged Kananda, Carl Rotolo, Laura Savino, Brian Owens, Eric A. Cravotto, Giancarlo RSC Adv Chemistry Nitrogen containing heterocycles are of immense research interest because they are often found as naturally occurring bioactive compounds. The prominence of N-heterocycles makes it vital to develop methods to increase their synthetic efficiencies and probe the effects of their modifications on biological efficacy. Medicinal chemists have exploited microwave-assisted organic synthesis (MAOS) to facilitate the development of complex heterocyclic structures. MAOS is a growing synthetic methodology among medicinal chemists and has proven to be more efficient in terms of reaction yield, reaction time, product purity and environmental friendliness for many reactions when compared to conventional thermal methods for cycloaddition and selective functionalization. The importance of nitrogen containing ring systems in medicine cannot be understated, as such ring systems have shown to be applicable in compounds such as vitamins, herbicides, anti-fungal agents, anti-bacterial agents and anti-cancer agents, among other things. The significance of these applications has created an unprecedented need for more efficient synthetic methods. This review presents an overview of MAOS and its role in recent and pressing advancements for the synthesis of small- and medium-sized nitrogen containing heterocycles, including pyrroles, indoles, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with medicinal uses. The Royal Society of Chemistry 2020-04-07 /pmc/articles/PMC9051880/ /pubmed/35498463 http://dx.doi.org/10.1039/d0ra01378a Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by/3.0/
spellingShingle Chemistry
Henary, Maged
Kananda, Carl
Rotolo, Laura
Savino, Brian
Owens, Eric A.
Cravotto, Giancarlo
Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title_full Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title_fullStr Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title_full_unstemmed Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title_short Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
title_sort benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9051880/
https://www.ncbi.nlm.nih.gov/pubmed/35498463
http://dx.doi.org/10.1039/d0ra01378a
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