Pub Date : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p347
Kapilkumar Galachar, Ashok Rathod, C. Pashavan, Y. Naliapara, Vipul Kataria, S. Korgaokar
The analogs of nitrogen-based heterocycles occupy an exclusive position as a value of more than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. Among many N-containing heterocycles, quinolines have become important due to their variety of applications in medicinal, synthetic organic chemistry as well as in the field of industrial chemistry. Present work gives information about the green and clean synthesis using multicomponent reactions (MCRs) methods and L-proline and ammonium acetate as a catalyst for the synthesis of quinoline derivatives. Synthesized quinoline derivatives undergo spectroscopic analysis and their biological evaluation.
{"title":"A Greener Approach for Synthesis of Quinoline-3-carboxylate\u0000Building Block and their Biological Screening","authors":"Kapilkumar Galachar, Ashok Rathod, C. Pashavan, Y. Naliapara, Vipul Kataria, S. Korgaokar","doi":"10.14233/ajomc.2021.ajomc-p347","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p347","url":null,"abstract":"The analogs of nitrogen-based heterocycles occupy an exclusive position as a value of more than 75%\u0000of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic\u0000moieties. Among many N-containing heterocycles, quinolines have become important due to their\u0000variety of applications in medicinal, synthetic organic chemistry as well as in the field of industrial\u0000chemistry. Present work gives information about the green and clean synthesis using multicomponent\u0000reactions (MCRs) methods and L-proline and ammonium acetate as a catalyst for the synthesis of\u0000quinoline derivatives. Synthesized quinoline derivatives undergo spectroscopic analysis and their\u0000biological evaluation.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81489973","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p352
P. S. Pawar, Sandip D. Gorshetwar, A. D. Kamble, Jotiram Chavan, G. G. Chougale, M. Patil, Satish M. Karpe
Water and zirconium(IV) as catalyst were found to be effective in the transformation of terminal aromatic alkyne to aromatic methyl ketone in the microwave. This terminal alkyne hydration reaction proceeded in excellent yield with Zr(cp)2Cl2. The reaction was moved efficiently in presence of electron donating or electron withdrawing substituent on aromatic ring. An eco-friendly synthesis of aldehyde by oxidative cleavage of nitroalkene was developed with Zr(cp)2Cl2 catalyst and water in microwave.
{"title":"Zr-Catalyzed Microwave Assisted Functionalization of Alkyne and Nitroalkene","authors":"P. S. Pawar, Sandip D. Gorshetwar, A. D. Kamble, Jotiram Chavan, G. G. Chougale, M. Patil, Satish M. Karpe","doi":"10.14233/ajomc.2021.ajomc-p352","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p352","url":null,"abstract":"Water and zirconium(IV) as catalyst were found to be effective in the transformation of terminal\u0000aromatic alkyne to aromatic methyl ketone in the microwave. This terminal alkyne hydration reaction\u0000proceeded in excellent yield with Zr(cp)2Cl2. The reaction was moved efficiently in presence of electron\u0000donating or electron withdrawing substituent on aromatic ring. An eco-friendly synthesis of aldehyde\u0000by oxidative cleavage of nitroalkene was developed with Zr(cp)2Cl2 catalyst and water in microwave.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76635804","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p354
Sarvesh Datta Dixit, Shalini Singh
Carbonic anhydrases, hCAs IX and XII are applied as the markers of progression of the disease in many oxygen deficient tumours and their specially manoeuvred inhibition is directly related to containing the growth of both primary tumours and tumour growth of secondary nature. Ligand-based quantitative structure-activity relationship (QSAR) studies were carried out on curcumin related, sulphonamide derivatives as inhibitors of human trans-membrane carbonic anhydrase isozyme, hCA IX by comparative molecular field similarity analysis (CoMSIA) implemented through the SYBYL package. The capacity of the model to predict coveted compound was evaluated using test set of three compounds. The best model created was found to be of choice as it showed a r2 value of 0.811 and a cross validated coefficient q2 value of 0.617 in tripos CoMSIA hydrophobic region. Results of the present study indicated that hydrophobic region factors play an important role in carbonic anhydrase hCA IX inhibition for compounds.
{"title":"in silico Modeling of Curcumin Based Sulfonamides Inhibitors of the Human\u0000trans-Membrane Carbonic Anhydrase Isozyme, hCA IX by CoMSIA","authors":"Sarvesh Datta Dixit, Shalini Singh","doi":"10.14233/ajomc.2021.ajomc-p354","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p354","url":null,"abstract":"Carbonic anhydrases, hCAs IX and XII are applied as the markers of progression of the disease in\u0000many oxygen deficient tumours and their specially manoeuvred inhibition is directly related to\u0000containing the growth of both primary tumours and tumour growth of secondary nature. Ligand-based\u0000quantitative structure-activity relationship (QSAR) studies were carried out on curcumin related,\u0000sulphonamide derivatives as inhibitors of human trans-membrane carbonic anhydrase isozyme, hCA\u0000IX by comparative molecular field similarity analysis (CoMSIA) implemented through the SYBYL\u0000package. The capacity of the model to predict coveted compound was evaluated using test set of three\u0000compounds. The best model created was found to be of choice as it showed a r2 value of 0.811 and a\u0000cross validated coefficient q2 value of 0.617 in tripos CoMSIA hydrophobic region. Results of the\u0000present study indicated that hydrophobic region factors play an important role in carbonic anhydrase\u0000hCA IX inhibition for compounds.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"87 10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87688061","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p344
Ashok Rathod, Kapilkumar Galachar, C. Pashavan, S. Korgaokar, Y. Naliapara
In current times, researchers adopted the click chemistry approach for the synthesis of various druglike molecules by using a few reliable, feasible, practical and selective chemical transformations via click formation. In present work, we focussed on the most triazole clubbed thiazolidine-2,4-dione derivatives as the most promising motifs for broad biological application. A total of fifteen (CF-4a-o) derivatives were synthesized and well characterized with various analytical techniques.
{"title":"Synthesis and Antimicrobial Activity of (Z)-2-(4-((5-((1-Benzylpiperidin-4-yl)methylene)-\u00002,4-dioxothiazolidin-3-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamides","authors":"Ashok Rathod, Kapilkumar Galachar, C. Pashavan, S. Korgaokar, Y. Naliapara","doi":"10.14233/ajomc.2021.ajomc-p344","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p344","url":null,"abstract":"In current times, researchers adopted the click chemistry approach for the synthesis of various druglike\u0000molecules by using a few reliable, feasible, practical and selective chemical transformations via\u0000click formation. In present work, we focussed on the most triazole clubbed thiazolidine-2,4-dione\u0000derivatives as the most promising motifs for broad biological application. A total of fifteen (CF-4a-o)\u0000derivatives were synthesized and well characterized with various analytical techniques.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90839910","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p315
Valmik S. Kapase
Several 1-substituted-3-aryl-1H-pyrazole-4-carbaldehyde (3a-g) derivatives were synthesized by substituted acetophenone (1a-d), substituted hydrazine (2a-b) and DMF in POCl3 and reaction mixture was irradiated with microwave at 20% power to furnish 1-substituted-3-aryl-1H-pyrazole-4-carbaldehydes derivatives (3a-g).
{"title":"Microwave Assisted Synthesis and QSAR Study of\u00001-Substituted-3-aryl-1H-pyrazole-4-carbaldehydes Derivatives","authors":"Valmik S. Kapase","doi":"10.14233/ajomc.2021.ajomc-p315","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p315","url":null,"abstract":"Several 1-substituted-3-aryl-1H-pyrazole-4-carbaldehyde (3a-g) derivatives were synthesized by substituted acetophenone (1a-d), substituted hydrazine (2a-b) and DMF in POCl3 and reaction mixture was irradiated with microwave at 20% power to furnish 1-substituted-3-aryl-1H-pyrazole-4-carbaldehydes derivatives (3a-g).","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"os-55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87373678","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p328
R. Wanare, Yogesh V. Punatkar, R. Jugade
7-Amino-3-methyl-5-(3′-aryl prop-2′-enoyl)-1,2-benzisoxazoles (2a-j) were synthesized by the condensation of 5-acetyl-7-amino-3-methyl-1,2-benzisoxazole (1) with aldehydes. The reaction of products 2a-j with urea produced 7-amino-3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazole derivatives (3a-j). Glucosylation of 3a-j with 2,3,4,6-tetra-O-acetyl glucuropyranosyl bromide (TAGBr) and tetrabutylammonium bromide (TBAB) gives corresponding glucosylated 7-amino-(β-D-2,3,4,6- tetra-O-acetyl glucopyranosyl)-3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazoles (4a-j). Glucosylated compounds 4a-j on deacetylation gives target products 7-amino-(β-D-glucopyranosyl)- 3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazoles (5a-j). Glucosylation and deacetylation reaction carried out by Knenigs-Knorr reaction. All the synthesized products were characterized by elemental analysis, IR, 1H NMR, 13C NMR and mass spectroscopy. The biological and electrochemical activities of all the synthesized compounds were also examined.
{"title":"Synthesis, Glucosylation and Polarographic Studies of Benzofused Pyrimidine Derivatives","authors":"R. Wanare, Yogesh V. Punatkar, R. Jugade","doi":"10.14233/ajomc.2021.ajomc-p328","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p328","url":null,"abstract":"7-Amino-3-methyl-5-(3′-aryl prop-2′-enoyl)-1,2-benzisoxazoles (2a-j) were synthesized by the condensation of 5-acetyl-7-amino-3-methyl-1,2-benzisoxazole (1) with aldehydes. The reaction of products 2a-j with urea produced 7-amino-3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazole derivatives (3a-j). Glucosylation of 3a-j with 2,3,4,6-tetra-O-acetyl glucuropyranosyl bromide (TAGBr) and tetrabutylammonium bromide (TBAB) gives corresponding glucosylated 7-amino-(β-D-2,3,4,6- tetra-O-acetyl glucopyranosyl)-3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazoles (4a-j). Glucosylated compounds 4a-j on deacetylation gives target products 7-amino-(β-D-glucopyranosyl)- 3-methyl-5-(4′-aryl-2′-pyrimidin-6′-yl)-1,2-benzisoxazoles (5a-j). Glucosylation and deacetylation reaction carried out by Knenigs-Knorr reaction. All the synthesized products were characterized by elemental analysis, IR, 1H NMR, 13C NMR and mass spectroscopy. The biological and electrochemical activities of all the synthesized compounds were also examined.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81951856","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p323
R. Singh, K. Srivastava, R. Tiwari, Jyoti Srivastava
The present work reports the synthesis of 4-(1-(substituted phenyl)-1H-naphtho[1,2-e][1,3]oxazin- 2(3H)-yl)-1-thia-4-azaspiro-[4.5]-decan-3-one IV(a-h) by 4-(((substituted phenyl)(2-hydroxynaphthalen- 1-yl) ethyl)amino)-1-thia-4-azaspiro[4.5]decan-3-one with formaldehyde in acetonitrile, containing a spiro ring obtained from the reaction of cyclohexylidene hydrazine and thioglycollic acid in DMF (cyclohexanone reacts with hydrazine hydrate in pyridine). The structures of the synthesized compounds have been established on the basis of elemental analysis, UV-vis absorption spectroscopy, IR, 1H NMR and mass spectral studies. The in vitro antimicrobial screening of all novel compounds was done against S. aureus, E. coli, P. aeruginosa and B. subtilis. The activity of compounds IVb, IVc, IVe and IVf compounds showed moderate to good activity against the tested microbes.
{"title":"Synthesis of Novel Oxazin Analogs of Thio-4-azaspiro[4.5]decan-3-one\u0000for their Antimicrobial Activity","authors":"R. Singh, K. Srivastava, R. Tiwari, Jyoti Srivastava","doi":"10.14233/ajomc.2021.ajomc-p323","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p323","url":null,"abstract":"The present work reports the synthesis of 4-(1-(substituted phenyl)-1H-naphtho[1,2-e][1,3]oxazin- 2(3H)-yl)-1-thia-4-azaspiro-[4.5]-decan-3-one IV(a-h) by 4-(((substituted phenyl)(2-hydroxynaphthalen- 1-yl) ethyl)amino)-1-thia-4-azaspiro[4.5]decan-3-one with formaldehyde in acetonitrile, containing a spiro ring obtained from the reaction of cyclohexylidene hydrazine and thioglycollic acid in DMF (cyclohexanone reacts with hydrazine hydrate in pyridine). The structures of the synthesized compounds have been established on the basis of elemental analysis, UV-vis absorption spectroscopy, IR, 1H NMR and mass spectral studies. The in vitro antimicrobial screening of all novel compounds was done against S. aureus, E. coli, P. aeruginosa and B. subtilis. The activity of compounds IVb, IVc, IVe and IVf compounds showed moderate to good activity against the tested microbes.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86242616","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p337
A. Gunjal, S. Katti
A novel series of 2,4,6-trisubstituted 1,4-dihydropyridine derivatives was designed and utilized for the computational studies for predicting absorption, distribution metabolism, elimination (ADME), pharmacological profile, toxicity and molecular docking of these derivatives. Some of the derivatives were found to have significant antihypertensive activity without toxicity.
{"title":"Design and in silico Evaluation of Some Pyridine Derivatives for Antihypertensive Activity","authors":"A. Gunjal, S. Katti","doi":"10.14233/ajomc.2021.ajomc-p337","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p337","url":null,"abstract":"A novel series of 2,4,6-trisubstituted 1,4-dihydropyridine derivatives was designed and utilized for the computational studies for predicting absorption, distribution metabolism, elimination (ADME), pharmacological profile, toxicity and molecular docking of these derivatives. Some of the derivatives were found to have significant antihypertensive activity without toxicity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87624597","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p321
H. Pandya, K. Joshi
A novel heterocyclic library were synthesized, characterized and tested for biological evaluation against bacteria and fungus. This novel series of substitute N-(4-(3-oxomorpholino)phenyl)-2-(4- ((phenylamino)-methyl)-1H-1,2,3-triazol-1-yl)acetamide via click chemistry approach in the presence of DMF:H2O:n-BuOH and CuSO4·5H2O in good yield. The title compounds have been synthesized with several structural variations. The synthesized compounds were screened for antimicrobial activity against standard drugs. The structure of synthesized compounds characterized by their spectral (IR, 1H NMR and mass) data. The purity of the synthesized compounds was confirmed by TLC.
{"title":"Synthesis, Characterization and Biological Evaluation of Some Novel Substitute\u0000N-(4-(3-Oxomorpholino)phenyl)-2-(4-((phenylamino)methyl)-1H-\u00001,2,3-triazol-1-yl)-acetamide via Click Chemistry Approach","authors":"H. Pandya, K. Joshi","doi":"10.14233/ajomc.2021.ajomc-p321","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p321","url":null,"abstract":"A novel heterocyclic library were synthesized, characterized and tested for biological evaluation against bacteria and fungus. This novel series of substitute N-(4-(3-oxomorpholino)phenyl)-2-(4- ((phenylamino)-methyl)-1H-1,2,3-triazol-1-yl)acetamide via click chemistry approach in the presence of DMF:H2O:n-BuOH and CuSO4·5H2O in good yield. The title compounds have been synthesized with several structural variations. The synthesized compounds were screened for antimicrobial activity against standard drugs. The structure of synthesized compounds characterized by their spectral (IR, 1H NMR and mass) data. The purity of the synthesized compounds was confirmed by TLC.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"69 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84358790","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 : 2021-01-01DOI: 10.14233/ajomc.2021.ajomc-p327
Mohan B. Kale, S. B. Jagtap, S. Devkate
The regioselective 1,4-addition reactions of copper thiocyanate catalyzed Grignard reagents to the substituted chalcones are reported. The homogeneous solution of dilithium tetrachloromanganate is used to transmetallate magnesium by using manganese. It adds regio-selectively to substituted chalcone derivatives and forms 1,4-addition products with higher yield under nitrogen atmosphere and at a lower temperature. It have been observed that manganese from dilithium tetrachloromanganate reagent replaces magnesium from Grignard reagent and adds regioselectively by 1,4-addition manner utilizing copper thiocyanate as a catalyst. The course of the reaction in the absence of dilithium tetrachloromanganate reagent was also studied and obtained a mixture of 1,2-addition and 1,4-addition products. In presence of dilithium tetrachloromanganate reagent, a good regio-selectivity and higher yield of desired 1,4-addition product were obtained. All the synthesized compounds were also evaluated for their antibacterial activity against Staphylococcus aureus (Gram-positive), Escherichia coli (Gramnegative) and antifungal activity against Aspergillus niger.
{"title":"Study of CuSCN Catalyzed Conjugate Addition Reactions of Grignard Reagents to\u0000Substituted Chalcones with Dilithium Tetrachloromanganate and their Biological Activities","authors":"Mohan B. Kale, S. B. Jagtap, S. Devkate","doi":"10.14233/ajomc.2021.ajomc-p327","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p327","url":null,"abstract":"The regioselective 1,4-addition reactions of copper thiocyanate catalyzed Grignard reagents to the substituted chalcones are reported. The homogeneous solution of dilithium tetrachloromanganate is used to transmetallate magnesium by using manganese. It adds regio-selectively to substituted chalcone derivatives and forms 1,4-addition products with higher yield under nitrogen atmosphere and at a lower temperature. It have been observed that manganese from dilithium tetrachloromanganate reagent replaces magnesium from Grignard reagent and adds regioselectively by 1,4-addition manner utilizing copper thiocyanate as a catalyst. The course of the reaction in the absence of dilithium tetrachloromanganate reagent was also studied and obtained a mixture of 1,2-addition and 1,4-addition products. In presence of dilithium tetrachloromanganate reagent, a good regio-selectivity and higher yield of desired 1,4-addition product were obtained. All the synthesized compounds were also evaluated for their antibacterial activity against Staphylococcus aureus (Gram-positive), Escherichia coli (Gramnegative) and antifungal activity against Aspergillus niger.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"35 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76747127","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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