scholarly journals The Impact of Microwave Irradiation Reaction in Medicinal Chemistry: A Review

2021 ◽  
Vol 37 (1) ◽  
pp. 01-24
Author(s):  
Ashutosh Pal ◽  
Krishnanka Shekhar Gayen
Keyword(s):  
Drug Discovery ◽  
Reaction Time ◽  
Microwave Irradiation ◽  
Medicinal Chemistry ◽  
Rapid Evolution ◽  
Therapeutic Agents ◽  
Conventional Heating ◽  
Compound Libraries ◽  
The Impact ◽  
Better Than

The present review collects an update of the reactions in the area of medicinal chemistry using microwave irradiation. This review come up with an overview of most salient reactions performed under microwave irradiation in the field of drug discovery. Moreover, chemists are preferring to use this reaction rapidly in the academic as well as pharmaceutical laboratory during their drug discovery and making library of compounds. This reaction is much greener using less amount and readily recyclable solvents or sometimes reaction process without solvents and product become much cleaner, often yields are better than the conventional heating. Microwave irradiation is now very robust instrument used in company in the field of drug discovery, due to reduce the reaction time from hour to minute or even second and efficiently creation of compound libraries through combinatorial methodology associated with drug discovery so that new therapeutic agents bring to the market quicker. Hopefully, we will observe in the future the use of microwave irradiation drugs for the patients and this technology will utilize increase in number extensively in the field of medicinal chemistry. As this is an exceedingly rapid evolution area, this review offers significant expertise to the interested readers.

scholarly journals Influence of Microwave Irradiation on Extraction of Chitosan from Shrimp Shell Waste

REAKTOR ◽  
2018 ◽  
Vol 18 (1) ◽  
pp. 45 ◽  
Author(s):  
Dwi Titik Apriyanti ◽  
Heru Susanto ◽  
Nur Rokhati
Keyword(s):  
Reaction Time ◽  
Microwave Irradiation ◽  
Raw Material ◽  
Conventional Heating ◽  
Health Food ◽  
Shrimp Shell ◽  
Shell Waste ◽  
Long Time ◽  
Shrimp Shell Waste ◽  
The Impact

Chitosan is natural polysaccharides which is nontoxic, biodegradable, and biocompatible and have many advantages in various kinds of fields including health, food, agriculture, and industry. Chitosan usually take long time to extract by conventional method for deacetylation process of chitin. Raw material for chitosan can be found in shrimp shell waste. Chitosan manufactures usually need high temperatures and chemicals in large quantities and it takes much time and consumes a lot of energy where will give bad effect to the environment. Recently microwave irradiation as nonconventional energy sources is widely used in chemical reactions. To reduce the impact of environmental pollution due to excessive use of chemical treatment, the objective of this work is processing chitosan under microwave irradiation. Expected production of chitosan with the same mass requires fewer chemicals than conventional heating. In particular, the study will examine the effect of making the chitosan and adding chemicals, reaction time and operating temperature and degree of deacetylation in chitosan with conventional heating methods that the results will be compared using a microwave. In this research will be developed to the design and fabrication of prototype scale extractor for manufacturing chitosan from shrimp shell waste after optimum results obtained from the research laboratory scale. From the research we can conclude that microwave will speed up reaction time. FTIR also showed functional group of chitosan formed from microwave irradiation have same results.  Keywords: chitosan, shrimp shells, microwave

scholarly journals THE INFLUENCES OF POWER VARIATIONS ON SELECTIVITY OF SYNTHESIS REACTION OF 2’-HYDROXYCHALCONE ANALOGUE UNDER MICROWAVE IRRADIATION

Molekul ◽  
2016 ◽  
Vol 11 (2) ◽  
pp. 299 ◽  
Author(s):  
Adel Zamri ◽  
Hilwan Yuda Teruna ◽  
Ihsan Ikhtiarudin
Keyword(s):  
Drug Discovery ◽  
Microwave Irradiation ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Synthesis Reaction ◽  
Material Synthesis ◽  
Power Variation ◽  
Material Chemistry ◽  
Irradiation Power

Some 2’-hydroxychalcone analogues have been widely used as an intermediate to synthesize various heterocyclic compounds, such as flavanones, flavanonols, flavones, flavonols and others. The heterocyclic compounds are also known to have a variety of interesting bioactivities in the medicinal chemistry and also have potency to be applied  in material chemistry including in industry. Therefore, 2’-hydroxychalcone analogues are often synthesized by researchers as intermediate, both in research associated with drug discovery and material synthesis. The aim of this study is to investigate the effect of microwave irradiation power variations on the selectivity of reaction of 2’-hydroxychalcone analogue synthesis. The variations of power that have been used in this study were 100, 180, 300 and 450 W with using a domestic microwave. Based on the study, we conclude that the power variation of microwave irradiationwere proven to effect the selectivity of synthesis reaction. In this study, the most suitable irradiation power to be applied on this synthesis is 180 W.

Comparison of Conventional and Microwave Synthesis of Phenyl-1H-pyrazoles and Phenyl-1H-pyrazoles-4-carboxylic Acid Derivatives

2021 ◽  
Vol 18 ◽  
Author(s):  
Antônio S. Machado ◽  
Flávio S. de Carvalho ◽  
Rayssa B.P. Mouraa ◽  
Lorrayne S. Chaves ◽  
Luciano M. Lião ◽  
...  
Keyword(s):  
Reaction Time ◽  
Carboxylic Acid ◽  
Pyrazole Ring ◽  
Conventional Heating ◽  
Pharmacological Activities ◽  
1H And 13C Nmr ◽  
Microwave Assisted ◽  
Attractive Option ◽  
Work Up ◽  
Better Than

Background: Molecules containing the pyrazole subunit considered that privileged scaffolds are of high importance due to their broad spectrum of pharmacological activities. For this reason, a method that is more efficient needs to be developed for the preparation of pyrazole derivatives. Objective: The purpose of this study was the optimisation of the conventional synthesis of the pyrazole ring and the oxidation of phenyl-1H-pyrazole-4-carbaldehyde to phenyl-1H-pyrazole-4-carboxylic acid through Microwave-Assisted Organic Synthesis (MAOS). Method: We performed a comparison between conventional synthesis and conventional synthesis with microwave heating using the synthesis of pyrazole ring described by Finar and Godfrey and, for the oxidation of phenyl-1H-pyrazole-4-carbaldehyde, the method described by Shriner and Kleiderer was used. Results: MAOS reduces the reaction time to obtain all compounds compared to conventional heating. At a temperature of 60°C, 5 minutes of reaction time, and power of 50W, the yield of phenyl-1H-pyrazoles (3a-m) compounds was in the range of 91 - 98% using MAOS, which is better than conventional heating (73 - 90%, 75ºC, 2 hours). An improvement in the yield for the oxidation reaction was also achieved with MAOS. The compounds (5a-m) were obtained with yields ranging from 62 - 92% (80ºC, 2 minutes, 150W), while the yields with conventional heating were in the range of 48 - 85% (80ºC, 1 hour). The 26 compounds were achieved through an easy work-up procedure with no chromatographic separation. The pure products were characterised by the spectral data obtained from IR, MS, 1H and 13C NMR or HSQC/HMBC techniques. Conclusion: The advantages of MAOS include short reaction time and increased yield, due to which it is an attractive option for the synthesis of pyrazole compounds.

First Sustainable Aziridination of Olefins Using Recyclable Copper-Immobilized Magnetic Nanoparticles

Synlett ◽  
2019 ◽  
Vol 30 (05) ◽  
pp. 563-566 ◽  
Author(s):  
Sylvestre Toumieux ◽  
Mohamad Khodadadi ◽  
Gwladys Pourceau ◽  
Matthieu Becuwe ◽  
Anne Wadouachi
Keyword(s):  
Magnetic Nanoparticles ◽  
Reaction Time ◽  
Microwave Irradiation ◽  
Significant Loss ◽  
Conventional Heating ◽  
Heating Method ◽  
Magnetic Extraction

The first copper-catalyzed aziridination of olefins using re­cyclable magnetic nanoparticles is described. Magnetic nanoparticles were modified with dopamine and used as a support to coordinate copper. The methodology was optimized with styrene as olefin and using [N-(p-toluenesulfonyl)imino]phenyliodinane (PhI=NTs) as nitrene source. A microwave irradiation decreased the reaction time by 4-fold compared to conventional heating method. The catalyst was recovered by simple magnetic extraction and could be reused successfully up to five times without significant loss of activity. The methodology was ­applied to a range of different olefins leading to moderate to excellent yields in the formation of the expected aziridine.

Synthesis of anti-inflammatory 2,3-unsaturated O-glycosides using conventional and microwave heating techniques

2017 ◽  
Vol 23 (3) ◽  
pp. 205-211
Author(s):  
Adriana Cristina N. de Melo ◽  
Ronaldo N. de Oliveira ◽  
João R. de Freitas Filho ◽  
Teresinha G. da Silva ◽  
Rajendra M. Srivastava
Keyword(s):  
Reaction Time ◽  
Microwave Irradiation ◽  
Microwave Heating ◽  
Acid Catalyst ◽  
Conventional Heating ◽  
Microwave Exposure ◽  
Ferrier Rearrangement ◽  
Acetyl Group ◽  
Anti Inflammatory

AbstractThe preparation of eight 2,3-unsaturated O-glycosides from D-glycals and alcohols, using montmorillonite K-10 as an acid catalyst, is described. The Ferrier rearrangement products were obtained in good yields using conventional heating and microwave irradiation but the reaction time was substantially reduced employing the latter procedure. The yields were slightly lower under microwave exposure. Five of the di-O-acetylated products were deacetylated to the glycosides in excellent yields. The acetylated products possess good anti-inflammatory property suggesting that the acetyl group plays an important role in reducing the inflammation. Among the compounds tested, glycosides containing thiophene as an aglycone present much better inflammation reducing characteristics than the analogues without this function.

Analogue-based drug discovery: Contributions to medicinal chemistry principles and drug design strategies. Microtubule stabilizers as a case in point (Special Topic Article)

2012 ◽  
Vol 84 (7) ◽  
pp. 1479-1542 ◽  
Author(s):  
Mohammad H. El-Dakdouki ◽  
Paul W. Erhardt
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Medicinal Chemistry ◽  
Drug Distribution ◽  
Therapeutic Agents ◽  
Special Topic ◽  
Design Strategies ◽  
Basic Principles ◽  
Research Activities ◽  
Alternative Drug

The benefits of utilizing marketed drugs as starting points to discover new therapeutic agents have been well documented within the IUPAC series of books that bear the title Analogue-based Drug Discovery (ABDD). Not as clearly demonstrated, however, is that ABDD also contributes to the elaboration of new basic principles and alternative drug design strategies that are useful to the field of medicinal chemistry in general. After reviewing the ABDD programs that have evolved around the area of microtubule-stabilizing chemo-therapeutic agents, the present article delineates the associated research activities that additionally contributed to general strategies that can be useful for prodrug design, identifying pharmacophores, circumventing multidrug resistance (MDR), and achieving targeted drug distribution.

scholarly journals In Situ Transesterification of Spirulina Microalgae to Produce Biodiesel Using Microwave Irradiation

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Alex K. Koech ◽  
Anil Kumar ◽  
Zachary O. Siagi
Keyword(s):  
Fatty Acid ◽  
Reaction Time ◽  
Microwave Irradiation ◽  
Spirulina Platensis ◽  
Reaction System ◽  
Conventional Heating ◽  
Process Conditions ◽  
In Situ Transesterification ◽  
Algae Biomass

The present technology of transesterification of vegetable oils to produce biodiesel, which is suited to replace petrodiesel, has economic challenges, and therefore, alternative sources are being explored. Microalgae, a renewable, third-generation biofuel resource, have the potential to become a viable feedstock due to their high oil content and environmentally friendly nature. The present study investigates the effect of microwave irradiation on the simultaneous extraction and transesterification of algae lipids to produce fatty acid methyl ester (FAME), in a batch reaction system using sulphuric acid catalyst. In situ transesterification combines the two steps of lipid extraction and transesterification into a single step. The microwave synthesis unit comprised of a 3-neck round bottom flask inside a 1300-Watt microwave oven, fitted with a quick-fit condenser and having an external stirrer. Response surface methodology (RSM) was used to analyse the influence of process variables, dry algae to methanol ratio 1 : 4 − 1 : 14   g / ml , algae biomass to catalyst ratio 1 : 0.0032 − 1 : 0.0368   wt % , and reaction time 1 − 11   min , at 500  rpm stirring rate for in situ reaction. FAME was analysed using gas chromatography (GC). The total lipid content of Arthrospira Spirulina platensis microalgae biomass was found to be 10.7 % by weight. The algae biomass also contained proteins at   51.83 % , moisture content at 7.8 % , and ash content 14.30 % by weight. RSM gave the optimum process conditions as dry algae biomass feed to methanol wt / vol ratio of 1 : 9, catalyst concentration of 2   wt % , and reaction time of   7   minutes   for a maximum FAME yield of 83.43   wt % . The major fatty acid composition of FAME was palmitic 43.83 % , linoleic   38.83 % , and linolenic 19.41 % . FAME properties obtained according to European Standards (EN 14214) and American Society for Testing and Materials (ASTM D 6751) standards were as follows: flash point 16 4 o C calorific value 32,911   kJ / kg , acid value 0.475 KOH / g , viscosity 4.45   m m 2 / s , and specific gravity   0.868 . The study showed that Arthrospira Spirulina platensis microalgae lipid FAME met the biodiesel standards (EN 14214 and ASTM D 6751) and has the potential to replace petrodiesel. Microwave irradiation increased the reaction rate resulting in a reduced reaction time of 7 minutes (as compared to 8 hours for conventional heating) and therefore was found to be a superior heating mode as compared to conventional heating.

scholarly journals A Green Synthesis of a Novel Calix[4]Resorcinarene from 7-Hydroxycitronellal Using Microwave Irradiation

2018 ◽  
Vol 18 (1) ◽  
pp. 53
Author(s):  
Ratnaningsih Eko Sardjono ◽  
Iqbal Musthapa ◽  
Iis Rosliana ◽  
Fitri Khoerunnisa ◽  
Galuh Yuliani
Keyword(s):  
Energy Consumption ◽  
Reaction Time ◽  
Microwave Irradiation ◽  
Irradiation Time ◽  
Microwave Oven ◽  
Conventional Heating ◽  
Heating Method ◽  
Microwave Assisted ◽  
Domestic Microwave Oven ◽  
Waste Production

A new versatile macromolecule cyclic C-3,7-dimethyl-7-hydroxycalix[4]resorcinarene (CDHHK4R) has been synthesized from a fragrance agent, 7-hydroxycitronellal, via microwave irradiation. The reaction utilized a domestic microwave oven at various irradiation time and power to yield an optimum condition. As a comparison, the conventional heating method was also employed for the synthesis of the same calix[4]resorcinarene. Compared to the conventional method, microwave-assisted reaction effectively reduced the reaction time, the amount of energy consumption and the waste production. It is found that the synthesis of CDHHK4R by microwave irradiation yielded 77.55% of product, higher than by conventional heating which was only 62.17%.

Nano Copper Catalyzed Microwave Assisted Coupling of Benzene Boronic Acids with Thiophenols

2019 ◽  
Vol 16 (6) ◽  
pp. 491-494
Author(s):  
Dinesh S. Gavhane ◽  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Shritesh D. Jagtap ◽  
Sajed H. Ansari ◽  
...  
Keyword(s):  
Reaction Time ◽  
Microwave Irradiation ◽  
Bond Formation ◽  
Boronic Acids ◽  
Conventional Heating ◽  
Microwave Technique ◽  
Microwave Assisted ◽  
Measurable Amount ◽  
Ligand Free

A proficient, microwave mediated methodology using CuFe2O4 nanoparticle as the catalyst for S-arylation of substituted benzene boronic acids with thiophenol has been developed. In this method, the substituted thioethers were easily obtained through a C-S bond formation using microwave irradiation technique as well as conventional heating in the presence of CuFe2O4 nanoparticles with modest to excellent yields with the less reaction time. The ligand free microwave technique helped in the preparation of substituted thioethers in measurable amount within 10 mins. The same results were obtained with conventional heating in 12h. The reported method is economically efficient and an alternative to the initial existing method for the preparation of substituted thioethers.

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