Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

Garella, Davide; Borretto, Emily; Stilo, Antonella Di; Martina, Katia; Cravotto, Giancarlo; Cintas, Pedro

doi:10.1039/c3md00152k

Cited by 80 publications

(24 citation statements)

References 89 publications

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“…The obtained data suggested that targeting MTB lipid metabolism pathways might provide an excellent route for attenuating or killing the bacterium [48]. The obtained data suggested that targeting MTB lipid metabolism pathways might provide an excellent route for attenuating or killing the bacterium [48].…”

Section: Five-membered Heterocycles With Two Heteroatomsmentioning

confidence: 87%

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Bandyopadhyay¹,

Banik²

2015

Green Synthetic Approaches for Biologically Relevant Heterocycles

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Section: Five-membered Heterocycles With Two Heteroatomsmentioning

confidence: 87%

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Bandyopadhyay¹,

Banik²

2015

Green Synthetic Approaches for Biologically Relevant Heterocycles

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“…We believe that the number of applications of MWs will increase manifold in the future. The use of MW‐assisted heterocyclic synthesis has been largely investigated by several research groups, and some reviews have already been published . So the MW‐assisted synthesis or green chemistry synthesis is more economical and highly environment friendly than conventional synthesis.…”

Section: Microwave‐assisted Organic Synthesesmentioning

confidence: 99%

Microwave‐activated Synthesis of Pyrroles: A Short Review

Sharma

Piplani

2015

Journal of Heterocyclic Chem

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In the current scenario for continuous requirement of better drugs, medicinal chemists must visage the challenging task of preparing novel patentable compounds, combining high activity and selectivity, good drug‐likeness, and pharmacokinetic properties. There is an acute need of new molecules in both lead identification and lead optimization. Chemists thoroughly scrutinize ways to simplify synthetic protocols using green chemistry approaches, for example, microwaves. Reduction in the reaction time by the use of microwaves has emerged as a promising method for bringing out new leads in organic synthesis. Among the azaheterocyclic systems, synthesis of pyrrole moiety has been a highly attractive and an inspiring proposition. It has been found to be an inbuilt pharmacophore of various momentous pharmacologically active compounds in medicinal chemistry. This article outlines the basic principles of microwave technology and its use in the synthesis of pyrrole derivatives wherein this technology has made a tremendous impact.

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“…These processes avoid the isolation and purification of intermediates, higher productivity, minimize solvent waste, and enhance the greenness of the transformations . Also, microwave‐assisted organic synthesis (MAOS) has become a very valuable tool, improving the outcome of multi‐component reactions because microwave heating is able to minimize side reactions, increase yields, reduce reaction times, improve reproducibility, and even enable inaccessible reactions by conventional heating and is particularly useful for the preparation of various biologically active heterocyclic compounds …”

Section: Introductionmentioning

confidence: 99%

“…[18,19] Also, microwave-assisted organic synthesis (MAOS) has become a very valuable tool, improving the outcome of multi-component reactions [20] because microwave heating is able to minimize side reactions, increase yields, reduce reaction times, improve reproducibility, and even enable inaccessible reactions by conventional heating and is particularly useful for the preparation of various biologically active heterocyclic compounds. [21] Therefore, the design of novel MCRs for the synthesis of diverse heterocycles has remained as an important topic for medicinal and organic chemists. The pyridine nucleus is one of the most popular N-heteroaromatics found in pharmaceuticals and natural products.…”

Section: Introductionmentioning

confidence: 99%

Nanomagnetically modified vitamin B₃ (Fe₃O₄@Niacin): An efficient and reusable green biocatalyst for microwave‐assisted rapid synthesis of 2‐amino‐3‐cyanopyridines in aqueous medium

Afradi

Pour

Dolat

et al. 2017

Applied Organom Chemis

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Superparamagnetic nanoparticles of modified vitamin B3 (Fe3O4@Niacin) represent a new, efficient and green biocatalyst for the one‐pot synthesis of 2‐amino‐3‐cyanopyridine derivatives via four‐component condensation reaction between aldehydes, ketones, malononitrile, and ammonium acetate under microwave irradiation in water. This new magnetic organocatalyst was easily isolated from the reaction mixture by magnetic decantation using an external magnet and reused at least six times without significant degradation in the activity. The catalyst was fully characterized by FT‐IR, XRD, SEM, VSM, UV–Vis, DLS and EDS. Excellent yield, very short reaction time (7–10 min), operational simplicity, easy work‐up procedure, avoidance of hazardous or toxic catalysts and organic solvents are the main advantages of this green methodology which makes it more economic than the other conventional methods.

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Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

Cited by 80 publications

References 89 publications

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Microwave‐activated Synthesis of Pyrroles: A Short Review

Nanomagnetically modified vitamin B₃ (Fe₃O₄@Niacin): An efficient and reusable green biocatalyst for microwave‐assisted rapid synthesis of 2‐amino‐3‐cyanopyridines in aqueous medium

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Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

Cited by 80 publications

References 89 publications

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Microwave-Induced Synthesis of Heterocycles of Medicinal Interests

Microwave‐activated Synthesis of Pyrroles: A Short Review

Nanomagnetically modified vitamin B3 (Fe3O4@Niacin): An efficient and reusable green biocatalyst for microwave‐assisted rapid synthesis of 2‐amino‐3‐cyanopyridines in aqueous medium

Contact Info

Product

Resources

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Nanomagnetically modified vitamin B₃ (Fe₃O₄@Niacin): An efficient and reusable green biocatalyst for microwave‐assisted rapid synthesis of 2‐amino‐3‐cyanopyridines in aqueous medium