Pub Date : 2022-08-20DOI: 10.2174/2213335609666220820153559
D. Karati, Dileep Kumar, K. Mahadik
The research aims to develop a sustainable microwave-assisted scheme for synthesizing 5-(benzylidene amino)-1-phenyl-1H-pyrazole-4-carbonitrile congeners. 5-(benzylideneamino)-1-phenyl-1H-pyrazole-4-carbonitrile scaffolds are novel molecules having various pharmacological activities such as neurodegenerative, anti-microbial, anti-cancer. Schiff base congeners are considered as efficient pharmacophores for research. These activities are due to the presence of azomethine (CH=N) group in the Schiff base compounds. To synthesise different novel Schiff base compounds of pyrazole nuclei by green chemistry with a decent yield. The 5-(benzylideneamino)-1-phenyl-1H-pyrazole-4-carbonitrile scaffolds were prepared by two step reactions. Both steps were microwave assisted. The first step was to synthesize 5-amino-1-phenyl-1H-pyrazole-4-carbonitrile as intermediate compound. This compound was synthesized by using phenyl hydrazine and 2-(ethoxymethylene)malononitrile. The temperature, pressure, and time required for this reaction were 1020C, 300W, and 45 minutes respectively. In the second step, the final Schiff base congeners were attained by reacting this compound with several aromatic aldehydes. The yield, reaction condition, and time consumption were all acceptable for the green synthetic methods rather than the conventional schemes. The microwave-assisted method was more efficient. The reactions were less time-consuming, and the overall yield of the all-synthesized compounds was 75-82%. Different spectroscopic methods characterized the synthesized congeners. The IR peak is considered the main functional group [azomethine] at 1611 cm-1 wavelength. This microwave-assisted synthetic scheme thus appears more environmentally due to a significant reduction in organic solvents, resulting in fewer hazardous residues. Using this scheme, we prepared different Schiff base congeners with satisfactory chemical yields
{"title":"Microwave Assisted Synthesis of a Novel Schiff Base Scaffolds of Pyrazole Nuclei: Green Synthetic Method","authors":"D. Karati, Dileep Kumar, K. Mahadik","doi":"10.2174/2213335609666220820153559","DOIUrl":"https://doi.org/10.2174/2213335609666220820153559","url":null,"abstract":"\u0000\u0000The research aims to develop a sustainable microwave-assisted scheme for synthesizing 5-(benzylidene amino)-1-phenyl-1H-pyrazole-4-carbonitrile congeners.\u0000\u0000\u0000\u00005-(benzylideneamino)-1-phenyl-1H-pyrazole-4-carbonitrile scaffolds are novel molecules having various pharmacological activities such as neurodegenerative, anti-microbial, anti-cancer. Schiff base congeners are considered as efficient pharmacophores for research. These activities are due to the presence of azomethine (CH=N) group in the Schiff base compounds.\u0000\u0000\u0000\u0000To synthesise different novel Schiff base compounds of pyrazole nuclei by green chemistry with a decent yield.\u0000\u0000\u0000\u0000The 5-(benzylideneamino)-1-phenyl-1H-pyrazole-4-carbonitrile scaffolds were prepared by two step reactions. Both steps were microwave assisted. The first step was to synthesize 5-amino-1-phenyl-1H-pyrazole-4-carbonitrile as intermediate compound. This compound was synthesized by using phenyl hydrazine and 2-(ethoxymethylene)malononitrile. The temperature, pressure, and time required for this reaction were 1020C, 300W, and 45 minutes respectively.\u0000In the second step, the final Schiff base congeners were attained by reacting this compound with several aromatic aldehydes. The yield, reaction condition, and time consumption were all acceptable for the green synthetic methods rather than the conventional schemes.\u0000\u0000\u0000\u0000The microwave-assisted method was more efficient. The reactions were less time-consuming, and the overall yield of the all-synthesized compounds was 75-82%. Different spectroscopic methods characterized the synthesized congeners. The IR peak is considered the main functional group [azomethine] at 1611 cm-1 wavelength.\u0000\u0000\u0000\u0000This microwave-assisted synthetic scheme thus appears more environmentally due to a significant reduction in organic solvents, resulting in fewer hazardous residues. Using this scheme, we prepared different Schiff base congeners with satisfactory chemical yields\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44405609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-18DOI: 10.2174/2213335609666220518100728
Krishnappa B Badiger, S. Khatavi, Kantharaju Kamanna
A variety of methods have been reported for the synthesis of pyrano[2,3-d]pyrimidines in the literature with some limitations, and generally used expensive catalysts, harmful solvent and prolonged reaction time. This paper describes an efficient and rapid multi-component synthesis of pyrano[2,3-d]pyrimidine through condensation of aromatic aldehyde, malononitrile and barbituric acid catalysed by agro-waste solvent catalyst under microwave irradiation. The present method provides several added advantages such as being environmentally friendly, simple work-up, inexpensive, and shorter reaction time affording excellent yields. The synthesized compounds were confirmed by various spectroscopic analysis such as FT-IR, 1H- & 13C-NMR and mass spectrometry. Develop an eco-friendly method for the synthesis of pyrano[2,3-d]pyrimidine derivatives. The pyrano[2,3-d]pyrimidine derivatives are prepared using an agro-waste-based catalyst, which avoids the use of the external base, additives and solvent in multi-component reactions. Further, the rate of the reaction is accelerated by custom-made microwave irradiation. The use of microwave irradiation showed many advantages over conventional methods such as reaction required less time, more yield and fewer by-products. Further, the custom-made microwave oven has the advantage of no spillage of any organic reagent or solvent to the microwave oven walls, because the reaction vessel is connected to a reflux condenser and direct exposure is avoided. We have selected Water Extract of Lemon Fruit Shell ash extract solvent as a greener homogenous organocatalysts, and reaction is accelerated by microwave irradiation for the inexpensive synthesis of pyrano[2,3-d]pyrimidine derivatives. In conclusion, we have developed a simple, efficient, agro-waste-based catalytic approach for the synthesis pyrano[2,3-d]pyrimidine derivatives employing WELFSA as an efficient agro-waste-based catalyst under microwave conditions. The method is found to added advantages of less hazardous, eco-friendly, metal-free, chemical-free, short reaction time, simple workup and isolated product in good to excellent yields.
{"title":"Microwave-Accelerated facile synthesis of pyrano[2,3-d]pyrimidine derivatives via one-pot strategy executed by agro-waste extract as a greener solvent media","authors":"Krishnappa B Badiger, S. Khatavi, Kantharaju Kamanna","doi":"10.2174/2213335609666220518100728","DOIUrl":"https://doi.org/10.2174/2213335609666220518100728","url":null,"abstract":"\u0000\u0000A variety of methods have been reported for the synthesis of pyrano[2,3-d]pyrimidines in the literature with some limitations, and generally used expensive catalysts, harmful solvent and prolonged reaction time. This paper describes an efficient and rapid multi-component synthesis of pyrano[2,3-d]pyrimidine through condensation of aromatic aldehyde, malononitrile and barbituric acid catalysed by agro-waste solvent catalyst under microwave irradiation. The present method provides several added advantages such as being environmentally friendly, simple work-up, inexpensive, and shorter reaction time affording excellent yields. The synthesized compounds were confirmed by various spectroscopic analysis such as FT-IR, 1H- & 13C-NMR and mass spectrometry.\u0000\u0000\u0000\u0000Develop an eco-friendly method for the synthesis of pyrano[2,3-d]pyrimidine derivatives.\u0000\u0000\u0000\u0000The pyrano[2,3-d]pyrimidine derivatives are prepared using an agro-waste-based catalyst, which avoids the use of the external base, additives and solvent in multi-component reactions. Further, the rate of the reaction is accelerated by custom-made microwave irradiation. The use of microwave irradiation showed many advantages over conventional methods such as reaction required less time, more yield and fewer by-products. Further, the custom-made microwave oven has the advantage of no spillage of any organic reagent or solvent to the microwave oven walls, because the reaction vessel is connected to a reflux condenser and direct exposure is avoided.\u0000\u0000\u0000\u0000We have selected Water Extract of Lemon Fruit Shell ash extract solvent as a greener homogenous organocatalysts, and reaction is accelerated by microwave irradiation for the inexpensive synthesis of pyrano[2,3-d]pyrimidine derivatives.\u0000\u0000\u0000\u0000In conclusion, we have developed a simple, efficient, agro-waste-based catalytic approach for the synthesis pyrano[2,3-d]pyrimidine derivatives employing WELFSA as an efficient agro-waste-based catalyst under microwave conditions. The method is found to added advantages of less hazardous, eco-friendly, metal-free, chemical-free, short reaction time, simple workup and isolated product in good to excellent yields.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42882998","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-16DOI: 10.2174/2213335609666220516112247
S. Avula, N. Rehman, R. Csuk, B. Das, A. Al‐Harrasi
A variety of natural products reveal the presence of the 1H-1,2,3-triazole moiety in their chemical structures. In general, these molecules also play a significant role in the agrochemical, medicinal and pharmaceutical industries. Microwave-asisted reactions have attracted great interest for researchers to synthesize 1H-1,2,3-triazole compounds in shorter times with increased yields. The objective of this study is to optimize the purity and yield of the product, shorter the reaction time, and make the reaction more eco-friendly with the help of microwave-assisted organic synthesis. The present work elucidates a very simple but efficient and rapid, highly productive synthesis of various substituted 1H-1,2,3-triazole series, using the Suzuki-Miyaura cross-coupling reaction, employing microwave irradiation in water, with tetrabutylammonium bromide (TBAB). Utilizing (S)- (-) ethyl lactate as the starting material, the synthesis of the substituted 1H-1,2,3-triazole aryl bromide (1) was achieved. This compound (1) was subjected to the Suzuki-Miyaura cross-coupling reaction under microwave irradiation, using a variety of aryl boronic acids in an aqueous medium, to attain high yields of the target products, namely 3a-w. Overall, this is an environmentally benign, very efficient technique under microwave-irradiations as a green and eco-friendly source. Only those methodologies that involve microwave-assisted reactions during synthesis in a related manner have been reviewed. Microwave-assisted Suzuki-Miyaura cross-coupling reactions in water of substituted 1H-1,2,3-triazole series can be employed to quickly explore and increase molecular diversity in synthetic chemistry. In this respect, microwave-mediated methods help researchers to make helpful studies.
{"title":"Microwave-Assisted: An Efficient Aqueous Suzuki-Miyaura Cross-Coupling Reaction of the Substituted 1H-1,2,3-Triazoles","authors":"S. Avula, N. Rehman, R. Csuk, B. Das, A. Al‐Harrasi","doi":"10.2174/2213335609666220516112247","DOIUrl":"https://doi.org/10.2174/2213335609666220516112247","url":null,"abstract":"\u0000\u0000A variety of natural products reveal the presence of the 1H-1,2,3-triazole moiety in their chemical structures. In general, these molecules also play a significant role in the agrochemical, medicinal and pharmaceutical industries. Microwave-asisted reactions have attracted great interest for researchers to synthesize 1H-1,2,3-triazole compounds in shorter times with increased yields.\u0000\u0000\u0000\u0000The objective of this study is to optimize the purity and yield of the product, shorter the reaction time, and make the reaction more eco-friendly with the help of microwave-assisted organic synthesis.\u0000\u0000\u0000\u0000The present work elucidates a very simple but efficient and rapid, highly productive synthesis of various substituted 1H-1,2,3-triazole series, using the Suzuki-Miyaura cross-coupling reaction, employing microwave irradiation in water, with tetrabutylammonium bromide (TBAB). Utilizing (S)- (-) ethyl lactate as the starting material, the synthesis of the substituted 1H-1,2,3-triazole aryl bromide (1) was achieved.\u0000\u0000\u0000\u0000This compound (1) was subjected to the Suzuki-Miyaura cross-coupling reaction under microwave irradiation, using a variety of aryl boronic acids in an aqueous medium, to attain high yields of the target products, namely 3a-w. Overall, this is an environmentally benign, very efficient technique under microwave-irradiations as a green and eco-friendly source. Only those methodologies that involve microwave-assisted reactions during synthesis in a related manner have been reviewed.\u0000\u0000\u0000\u0000Microwave-assisted Suzuki-Miyaura cross-coupling reactions in water of substituted 1H-1,2,3-triazole series can be employed to quickly explore and increase molecular diversity in synthetic chemistry. In this respect, microwave-mediated methods help researchers to make helpful studies.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43323366","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-04-14DOI: 10.2174/2213335609666220414141731
D. Karati, K. Mahadik, Dileep Kumar
The research work aims to develop sustainable microwave-assisted scheme for the synthesis of 4-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile congeners. 4-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile scaffolds are novel molecules having various pharmacological activities such as neurodegenerative, anti-microbial, anti-cancer. Schiff base congeners are considered as efficient pharmacophores for research. These activities are due to the presence of azomethine (CH=N) group in the Schiff base compounds. To synthesise different novel Schiff base scaffolds of pyrimidine nuclei by green chemistry with good yield. The 4-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile scaffolds were prepared by two step reactions. Both steps were microwave assisted. The first step was to synthesize 4-amino-6-phenylpyrimidine-5-carbonitrile as intermediate compound. This compound was synthesized by using benzaldehyde, malononitrile and formamidine hydrochloride. The reaction conditions are as following: temperature- 1010C, pressure- 300W, time- 50min. The final Schiff base congeners were obtained by reacting it with various aromatic aldehydes in the second step. The yield, reaction condition, and time consumption all were very acceptable for the green synthetic methods rather than the conventional schemes. Microwave assisted method was more efficient. The reactions were less time consuming and the overall yield of the all-synthesized compounds was in the range of 72-81%. The synthesized congeners were characterized by different spectroscopic methods. The main functional group [azomethine] was considered by the IR peak at 1611 cm-1 wavelength. This microwave assisted synthetic method thus emerges as more eco-friendly due to a much-reduced usage of organic solvents, leading to less harmful residues. Using this scheme, we synthesized different Schiff base congeners with satisfactory chemical yields.
{"title":"Microwave assisted synthetic scheme of a novel Schiff base congeners of pyrimidine nuclei by using water as solvent: green approach of synthesis","authors":"D. Karati, K. Mahadik, Dileep Kumar","doi":"10.2174/2213335609666220414141731","DOIUrl":"https://doi.org/10.2174/2213335609666220414141731","url":null,"abstract":"\u0000\u0000The research work aims to develop sustainable microwave-assisted scheme for the synthesis of 4-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile congeners.\u0000\u0000\u0000\u00004-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile scaffolds are novel molecules having various pharmacological activities such as neurodegenerative, anti-microbial, anti-cancer. Schiff base congeners are considered as efficient pharmacophores for research. These activities are due to the presence of azomethine (CH=N) group in the Schiff base compounds.\u0000\u0000\u0000\u0000To synthesise different novel Schiff base scaffolds of pyrimidine nuclei by green chemistry with good yield.\u0000\u0000\u0000\u0000The 4-(benzylidene amino)-6-phenylpyrimidine-5-carbonitrile scaffolds were prepared by two step reactions. Both steps were microwave assisted. The first step was to synthesize 4-amino-6-phenylpyrimidine-5-carbonitrile as intermediate compound. This compound was synthesized by using benzaldehyde, malononitrile and formamidine hydrochloride. The reaction conditions are as following: \u0000temperature- 1010C, pressure- 300W, time- 50min.\u0000The final Schiff base congeners were obtained by reacting it with various aromatic aldehydes in the second step. The yield, reaction condition, and time consumption all were very acceptable for the green synthetic methods rather than the conventional schemes.\u0000\u0000\u0000\u0000Microwave assisted method was more efficient. The reactions were less time consuming and the overall yield of the all-synthesized compounds was in the range of 72-81%. The synthesized congeners were characterized by different spectroscopic methods. The main functional group [azomethine] was considered by the IR peak at 1611 cm-1 wavelength.\u0000\u0000\u0000\u0000This microwave assisted synthetic method thus emerges as more eco-friendly due to a much-reduced usage of organic solvents, leading to less harmful residues. Using this scheme, we synthesized different Schiff base congeners with satisfactory chemical yields.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48323164","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-24DOI: 10.2174/2213335609666220324144409
Subhraraj Panda
Ultrasonic research can be used to recognise molecular connections and structural behaviour of molecules. The combination of ultrasonic velocity, density, and viscosity data provides a plethora of information on ion interactions, dipoles, hydrogen bonding, multi-polar, and dispersive forces. To find out the molecular interaction of solute dextran of different concentration with distilled water as a solvent. The “ultrasonic speed (U), density (ρ), and viscosity (η)” at 323 K have been determined at four different frequencies, i.e.“1MHz,5MHz,9MHz and 12 MHz”. The derived acoustical parameters such as “acoustic impedance (Z), adiabatic compressibility (β), intermolecular free length (Lf), relaxation time (τ), Gibb’s free energy (ΔG)” have been determined from the experimental data. The significance gives subjective data with respect to nature and quality of the particles interactions between solute and solvent in the liquids solutions. To measure the density by specific gravity bottle, viscosity by Ostwald’s viscometer and ultrasonic velocity through ultrasonic interferometer of the solution and to calculate the thermo acoustical parameters using the measured parameters. Ultrasonic wave propagation affects the physical properties of the medium and hence furnishes information on the physics of liquid and solution. The measured parameters like ultrasonic velocity, density, and viscosity have been used to understand the solute-solute and solute-solvent interactions in the solution containing dextran with water. The effect of frequency on thermo acoustical parameters has been studied. From the above studies, the nature of forces between molecules such as hydrogen bonds, charge transfer complexes, breaking of hydrogen bonds and complexes has been interpreted.
{"title":"Analysis of Aqueous Dextran: An Ultrasonic Studies","authors":"Subhraraj Panda","doi":"10.2174/2213335609666220324144409","DOIUrl":"https://doi.org/10.2174/2213335609666220324144409","url":null,"abstract":"\u0000\u0000Ultrasonic research can be used to recognise molecular connections and structural behaviour of molecules. The combination of ultrasonic velocity, density, and viscosity data provides a plethora of information on ion interactions, dipoles, hydrogen bonding, multi-polar, and dispersive forces.\u0000\u0000\u0000\u0000To find out the molecular interaction of solute dextran of different concentration with distilled water as a solvent. The “ultrasonic speed (U), density (ρ), and viscosity (η)” at 323 K have been determined at four different frequencies, i.e.“1MHz,5MHz,9MHz and 12 MHz”. The derived acoustical parameters such as “acoustic impedance (Z), adiabatic compressibility (β), intermolecular free length (Lf), relaxation time (τ), Gibb’s free energy (ΔG)” have been determined from the experimental data. The significance gives subjective data with respect to nature and quality of the particles interactions between solute and solvent in the liquids solutions.\u0000\u0000\u0000\u0000To measure the density by specific gravity bottle, viscosity by Ostwald’s viscometer and ultrasonic velocity through ultrasonic interferometer of the solution and to calculate the thermo acoustical parameters using the measured parameters.\u0000\u0000\u0000\u0000Ultrasonic wave propagation affects the physical properties of the medium and hence furnishes information on the physics of liquid and solution. The measured parameters like ultrasonic velocity, density, and viscosity have been used to understand the solute-solute and solute-solvent interactions in the solution containing dextran with water.\u0000\u0000\u0000\u0000The effect of frequency on thermo acoustical parameters has been studied. From the above studies, the nature of forces between molecules such as hydrogen bonds, charge transfer complexes, breaking of hydrogen bonds and complexes has been interpreted.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45252746","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-24DOI: 10.2174/2213335609666220324145341
F. Norouzi, N. Foroughifar, A. Khajeh-Amiri, H. Pasdar
Choline Chloride - Thiourea / Sulfuric Acid is a powerful and efficient green catalyst used for one-pot synthesis of quinazoline-4 (3H) -one derivatives via a reaction between various amines, acetic anhydride, and anthranilic acid under microwave irradiation and solvent-free conditions (4a-q). Microwave irradiation, which is a faster, more cost-effective, less energy-intensive, and more efficient method than conventional heating, has been used to synthesize some quinazolinone derivatives. For the past ten years, one of the major subjects in synthetic organic chemistry has been green synthesis, which has used efficient and environmentally friendly methods to synthesize biological compounds. The use of catalysts has significant advantages, including ease of preparation and separation, chemical and thermal stability, and environmental friendliness due to features such as reusability, low cost, and efficient, easy workup techniques. Therefore, the mechanism is performed by a non-toxic organic catalyst that uses the least energy and chemical reactants in accordance with the principles of green chemistry and least waste. One-pot and sequential addition methods have been used to synthesize quinazolinone derivatives. In the sequential addition method, the reaction was started by adding acetic anhydride and anthranilic acid to the reaction vessel under microwave irradiation and continued by adding choline chloride thiourea / sulfuric acid as efficient recyclable green catalysts and the desired amine. In vitro, the well diffusion method against different pathogenic strains was used to evaluate the antimicrobial activity of quinazoline-4 (3H) -one derivatives. Pathogenic strains used were Candida albicans ATCC 10231 (yeast), Aspergillus niger ATCC 16404 (fungus), Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027 (bacteria) and ATCC 6538, and Staphylococcus aureus S. epidermidis ATCC 12228. Pyrimidine-containing compounds in which the 3-hydroxyl, 2,5-Dimethoxy, 4-bromo, 4 ‐ Methoxy, and 4 ‐ chloro groups are attached to the phenyl ring of pyrimidine exhibit antimicrobial properties. In a short reaction time, a variety of biologically active quinazolinone derivatives were synthesized with a high efficiency. According to the results, it was found that with aliphatic amines, the reaction time was shorter and the reaction efficiency was higher. Products synthesized from aromatic amines had more antibacterial properties. In this work, a variety of 2-methyl-quinazoline-4 (3H) -one derivatives (4a–q) were synthesized as potent antibacterial agents under microwave irradiation and solvent-free conditions in the presence of ChCl-thiourea / H2SO4 as an efficient, eco-friendly, and recyclable catalyst.
{"title":"A novel powerful Choline Chloride – Thiourea /Sulfuric Acid, efficient and recyclable catalyst via microwave‐assisted for the synthesis of Quinazolin- 4(3H)–one derivatives as Antibacterial Agents in green media","authors":"F. Norouzi, N. Foroughifar, A. Khajeh-Amiri, H. Pasdar","doi":"10.2174/2213335609666220324145341","DOIUrl":"https://doi.org/10.2174/2213335609666220324145341","url":null,"abstract":"\u0000\u0000Choline Chloride - Thiourea / Sulfuric Acid is a powerful and efficient green catalyst used for one-pot synthesis of quinazoline-4 (3H) -one derivatives via a reaction between various amines, acetic anhydride, and anthranilic acid under microwave irradiation and solvent-free conditions (4a-q). Microwave irradiation, which is a faster, more cost-effective, less energy-intensive, and more efficient method than conventional heating, has been used to synthesize some quinazolinone derivatives.\u0000\u0000\u0000\u0000For the past ten years, one of the major subjects in synthetic organic chemistry has been green synthesis, which has used efficient and environmentally friendly methods to synthesize biological compounds. The use of catalysts has significant advantages, including ease of preparation and separation, chemical and thermal stability, and environmental friendliness due to features such as reusability, low cost, and efficient, easy workup techniques. Therefore, the mechanism is performed by a non-toxic organic catalyst that uses the least energy and chemical reactants in accordance with the principles of green chemistry and least waste.\u0000\u0000\u0000\u0000One-pot and sequential addition methods have been used to synthesize quinazolinone derivatives. In the sequential addition method, the reaction was started by adding acetic anhydride and anthranilic acid to the reaction vessel under microwave irradiation and continued by adding choline chloride thiourea / sulfuric acid as efficient recyclable green catalysts and the desired amine. In vitro, the well diffusion method against different pathogenic strains was used to evaluate the antimicrobial activity of quinazoline-4 (3H) -one derivatives. Pathogenic strains used were Candida albicans ATCC 10231 (yeast), Aspergillus niger ATCC 16404 (fungus), Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027 (bacteria) and ATCC 6538, and Staphylococcus aureus S. epidermidis ATCC 12228. Pyrimidine-containing compounds in which the 3-hydroxyl, 2,5-Dimethoxy, 4-bromo, 4 ‐ Methoxy, and 4 ‐ chloro groups are attached to the phenyl ring of pyrimidine exhibit antimicrobial properties.\u0000\u0000\u0000\u0000In a short reaction time, a variety of biologically active quinazolinone derivatives were synthesized with a high efficiency. According to the results, it was found that with aliphatic amines, the reaction time was shorter and the reaction efficiency was higher. Products synthesized from aromatic amines had more antibacterial properties.\u0000\u0000\u0000\u0000In this work, a variety of 2-methyl-quinazoline-4 (3H) -one derivatives (4a–q) were synthesized as potent antibacterial agents under microwave irradiation and solvent-free conditions in the presence of ChCl-thiourea / H2SO4 as an efficient, eco-friendly, and recyclable catalyst.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45890532","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The study effect of microwave radiation on the catalytic properties of transition metal ferrites synthesized by ceramic and sol-gel methods, in the oxidation reaction of carbon monoxide into dioxide. The aim of this work is to study the effect of microwave radiation on the production of cobalt, copper, nickel and manganese ferrites by sol-gel combustion technology using various organic reagents and to study their catalytic activity in the oxidative conversion of carbon monoxide into dioxide. Microwave treatment was carried out on a setup based on an EM-G5593V microwave oven (Panasonic) with a magnetron power varying from 300 to 800 W with an operating frequency of 2450 MHz. X-ray phase analysis of the products was carried out on a Bruker D 2Phazer automatic diffractometer. The measurement of the specific surface area of the samples was determined by low-temperature nitrogen adsorption by the multipoint BET method on a SORBI-MS instrument (ZAO META, Russia). IR spectra were recorded using FT-IR LUMOS Bruker spectrometers. The micrographs of samples were analyzed on the Sigma VP (Carl Zeiss Jena) equipment. It was determined that the most active catalysts for the oxidation of carbon monoxide to dioxide are ferrites obtained by the sol-gel combustion method using microwave radiation to "ignite" the gel. The use of microwave radiation in the preparation of ferrites by the sol-gel method with combustion can, in a very short time, measured in seconds, initiate a self-propagating exothermic combustion reaction in the entire volume of the sample. The catalytic activity in the oxidative conversion of carbon monoxide obtained by this method of ferrites comparable to the activity of ferrites obtained by the sol-gel method with traditional combustion.
{"title":"Microwave Sol-Gel Synthesis of Co, Ni, Cu, Mn Ferrites and İnvestigation of Their Activity in the Oxidation Reaction of Carbon Monoxide","authors":"Zulfugarova Sima Mamed, Azimova Gunel Ramiz, Aleskerova Zuleyxa Fikret, Ismailov Etibar Humbat, Litvishkov Yuriy Nikolayevich, Tagiyev Dilqam Babir","doi":"10.2174/2213335609666220303105233","DOIUrl":"https://doi.org/10.2174/2213335609666220303105233","url":null,"abstract":"\u0000\u0000The study effect of microwave radiation on the catalytic properties of transition metal ferrites synthesized by ceramic and sol-gel methods, in the oxidation reaction of carbon monoxide into dioxide.\u0000\u0000\u0000\u0000The aim of this work is to study the effect of microwave radiation on the production of cobalt, copper, nickel and manganese ferrites by sol-gel combustion technology using various organic reagents and to study their catalytic activity in the oxidative conversion of carbon monoxide into dioxide.\u0000\u0000\u0000\u0000Microwave treatment was carried out on a setup based on an EM-G5593V microwave oven (Panasonic) with a magnetron power varying from 300 to 800 W with an operating frequency of 2450 MHz. X-ray phase analysis of the products was carried out on a Bruker D 2Phazer automatic diffractometer. The measurement of the specific surface area of the samples was determined by low-temperature nitrogen adsorption by the multipoint BET method on a SORBI-MS instrument (ZAO META, Russia). IR spectra were recorded using FT-IR LUMOS Bruker spectrometers. The micrographs of samples were analyzed on the Sigma VP (Carl Zeiss Jena) equipment.\u0000\u0000\u0000\u0000It was determined that the most active catalysts for the oxidation of carbon monoxide to dioxide are ferrites obtained by the sol-gel combustion method using microwave radiation to \"ignite\" the gel.\u0000\u0000\u0000\u0000The use of microwave radiation in the preparation of ferrites by the sol-gel method with combustion can, in a very short time, measured in seconds, initiate a self-propagating exothermic combustion reaction in the entire volume of the sample. The catalytic activity in the oxidative conversion of carbon monoxide obtained by this method of ferrites comparable to the activity of ferrites obtained by the sol-gel method with traditional combustion.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46855512","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-18DOI: 10.2174/2213335609666220118102344
Kaushik N. Kundaliya, N. Patel, D. I. Brahmbhatt
The 1,2,3-triazole, pyrazole and coumarin based derivatives have received much attention due to their wide coverage of biological properties. The present work describes the microwave synthesis of novel triazolyl pyrazolyl pyrazoline substituted coumarins. Structure of all the newly synthesized compounds are characterized by spectral analysis and screened for their in vitro antimicrobial activity by Broth dilution method. In synthetic method , the targets were prepared by reaction of various 3-{3-[3-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazol-4-yl]acryloyl} coumarins (coumarin chalcones) (3a-d) with hydrazine hydrate or aryl hydrazine(5a-c) in the presence of acetic/propionic acid under microwave irradiation. The structures of all the synthesized compounds were established by IR, 1H-NMR, 13C-APT and selected mass spectral data. The target compounds were also screen for their in vitro antimicrobial efficiency against representative panel of pathogenic strains specifically Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis), Gram-negative bacteria (Escherichia coli, Salmonella typhi) and Fungi (Candida albicans, Aspergillus niger). In conclusion ,the target compounds were obtained by Microwave Irradiation (MWI) technique in good yield with short reaction time. Among all the synthesized compounds ,4c,4h,6a,6h and 6l were found to have significant activity against bacterial and fungal strains.
{"title":"Microwave Assisted Synthesis of Novel Triazolyl Pyrazolyl Pyrazoline Substituted Coumarins and their Antimicrobial Activity","authors":"Kaushik N. Kundaliya, N. Patel, D. I. Brahmbhatt","doi":"10.2174/2213335609666220118102344","DOIUrl":"https://doi.org/10.2174/2213335609666220118102344","url":null,"abstract":"\u0000\u0000The 1,2,3-triazole, pyrazole and coumarin based derivatives have received much attention due to their wide coverage of biological properties. The present work describes the microwave synthesis of novel triazolyl pyrazolyl pyrazoline substituted coumarins. Structure of all the newly synthesized compounds are characterized by spectral analysis and screened for their in vitro antimicrobial activity by Broth dilution method.\u0000\u0000\u0000\u0000In synthetic method , the targets were prepared by reaction of various 3-{3-[3-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazol-4-yl]acryloyl} coumarins (coumarin chalcones) (3a-d) with hydrazine hydrate or aryl hydrazine(5a-c) in the presence of acetic/propionic acid under microwave irradiation.\u0000\u0000\u0000\u0000The structures of all the synthesized compounds were established by IR, 1H-NMR, 13C-APT and selected mass spectral data. The target compounds were also screen for their in vitro antimicrobial efficiency against representative panel of pathogenic strains specifically Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis), Gram-negative bacteria (Escherichia coli, Salmonella typhi) and Fungi (Candida albicans, Aspergillus niger).\u0000\u0000\u0000\u0000In conclusion ,the target compounds were obtained by Microwave Irradiation (MWI) technique in good yield with short reaction time. Among all the synthesized compounds ,4c,4h,6a,6h and 6l were found to have significant activity against bacterial and fungal strains.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2022-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47339790","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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