An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothi...An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothiocyanates,amines and cyclic ethers.This methodology features simple operation,mild reaction conditions,favorable functional group tolerance,easily available starting materials and high efficiency.展开更多
An efficient synthetic protocol for the 1,4-diaryl-1,4-dihydropyridines was developed via the domino four-component reaction of arylamine,acetylenedicarboxylate,aromatic aldehyde and ethyl acetoacetate.The reaction me...An efficient synthetic protocol for the 1,4-diaryl-1,4-dihydropyridines was developed via the domino four-component reaction of arylamine,acetylenedicarboxylate,aromatic aldehyde and ethyl acetoacetate.The reaction mechanism involves the formation of β-enamino ester and its sequential Michael addition to arylidene acetoacetate.展开更多
A mild and efficient synthesis of N-substituted-3-aryl-3-（2-hydroxy-4,4-dimethyl-6-oxocyclohex-l- enyl）propanamides via four-component reaction of an aldehyde, amine, Meldrum＇s acid and 5,5-dimethylcyclo- hexane-1,...A mild and efficient synthesis of N-substituted-3-aryl-3-（2-hydroxy-4,4-dimethyl-6-oxocyclohex-l- enyl）propanamides via four-component reaction of an aldehyde, amine, Meldrum＇s acid and 5,5-dimethylcyclo- hexane-1,3-dione in the presence of benzyltriethylammonium chloride （TEBAC） in aqueous medium is described. This method has the advantages of accessible starting materials, good yields, mild reaction conditions and eco- friendliness.展开更多
An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot,four-component reaction of 4-hydroxycoumarin, formaldehyde,cyclohexanedione,ammonium ceric nitrate under microwave irradiation was accomplishe...An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot,four-component reaction of 4-hydroxycoumarin, formaldehyde,cyclohexanedione,ammonium ceric nitrate under microwave irradiation was accomplished.The structures of these compounds were unambiguously confirmed by single crystal X-ray diffraction.Furthermore,the anti-AChE activities of these compounds in vitro were investigated at concentrations of 20μM and 50μM by using a standard Ellman's method.The relationship of inhibitory activities and structures of these chromeno [4,3-b]quinolines was also systematically studied.Of all the compounds investigated,4ag emerged as the most potent AChE inhibitor with IC50 values of 5.63μM,and it might be used as potent lead for the development anti-AChE agents.Moreover,molecular modelling was conducted to understand the optimal interaction of AChE with these types of compounds.展开更多
Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was t...Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was tested by solid-phase synthesis. The Fmoc protected PNA monomer was build up with thymin-1-yl acetic acid, 3-methylbutyl aldehyde, Fmoc protected aminoethyl isocyanide and Gly-Wang resin.展开更多
An efficient and straightforward procedure has been developed for the synthesis of highly substituted mono- and bis-N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates via a one-pot, four-component domino reaction of ami...An efficient and straightforward procedure has been developed for the synthesis of highly substituted mono- and bis-N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates via a one-pot, four-component domino reaction of amines, dialkyl acetylenedicarboxylates and formaldehyde in the presence of InCl3 （20 mol%） in MeOH at ambient temperature. The salient advantages of this method are mild reaction conditions, environmentally benign, high to excellent yields, shorter reaction times, easy operation and no column chromatographic separation.展开更多
A microwave mediated solvent free one pot synthesis of formazans is developed using the solid acid, KHSO4. The products were obtained in a short reaction time in high yield. This study was undertaken to find an altern...A microwave mediated solvent free one pot synthesis of formazans is developed using the solid acid, KHSO4. The products were obtained in a short reaction time in high yield. This study was undertaken to find an alternative and green method for the synthesis of formazans in the absence of corrosive mineral acids, buffered solutions and volatile organic compounds (VOCs).展开更多
基金financially supported by Natural Science Foundation of Shandong Province(No.ZR2021MB065)the major innovation fund of Shandong Province(No.2021ZDSYS_(2)3)the National Natural Science Foundation of China(Nos.21976105,22101237).
文摘An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothiocyanates,amines and cyclic ethers.This methodology features simple operation,mild reaction conditions,favorable functional group tolerance,easily available starting materials and high efficiency.
基金Supported by the National Natural Science Foundation of China(No.20972132)the Fund of Key Laboratory of Environmental Resource and Material,Jiangsu Province,China
文摘An efficient synthetic protocol for the 1,4-diaryl-1,4-dihydropyridines was developed via the domino four-component reaction of arylamine,acetylenedicarboxylate,aromatic aldehyde and ethyl acetoacetate.The reaction mechanism involves the formation of β-enamino ester and its sequential Michael addition to arylidene acetoacetate.
文摘A mild and efficient synthesis of N-substituted-3-aryl-3-（2-hydroxy-4,4-dimethyl-6-oxocyclohex-l- enyl）propanamides via four-component reaction of an aldehyde, amine, Meldrum＇s acid and 5,5-dimethylcyclo- hexane-1,3-dione in the presence of benzyltriethylammonium chloride （TEBAC） in aqueous medium is described. This method has the advantages of accessible starting materials, good yields, mild reaction conditions and eco- friendliness.
基金NSFC(Grant No.81773557,81573279,81373255)Major Project of Technology Innovation Program of Hubei Province(Grant No.2016ACA126)+1 种基金NSFHP(Grant No.2017CFA024)and the Fun damental Research Funds for the Central Universities of China(Grant No.2042017kf0288)
文摘An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot,four-component reaction of 4-hydroxycoumarin, formaldehyde,cyclohexanedione,ammonium ceric nitrate under microwave irradiation was accomplished.The structures of these compounds were unambiguously confirmed by single crystal X-ray diffraction.Furthermore,the anti-AChE activities of these compounds in vitro were investigated at concentrations of 20μM and 50μM by using a standard Ellman's method.The relationship of inhibitory activities and structures of these chromeno [4,3-b]quinolines was also systematically studied.Of all the compounds investigated,4ag emerged as the most potent AChE inhibitor with IC50 values of 5.63μM,and it might be used as potent lead for the development anti-AChE agents.Moreover,molecular modelling was conducted to understand the optimal interaction of AChE with these types of compounds.
基金This work was supposed by the National Basic Research Program(973 Program)from the Ministry of Science and Technology of China(G1998051114)the National Natural Science Foundation of China(20272004)
文摘Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was tested by solid-phase synthesis. The Fmoc protected PNA monomer was build up with thymin-1-yl acetic acid, 3-methylbutyl aldehyde, Fmoc protected aminoethyl isocyanide and Gly-Wang resin.
基金support from the Research Council of University of Sistan and Baluchestan and Payame Noor University
文摘An efficient and straightforward procedure has been developed for the synthesis of highly substituted mono- and bis-N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates via a one-pot, four-component domino reaction of amines, dialkyl acetylenedicarboxylates and formaldehyde in the presence of InCl3 （20 mol%） in MeOH at ambient temperature. The salient advantages of this method are mild reaction conditions, environmentally benign, high to excellent yields, shorter reaction times, easy operation and no column chromatographic separation.
文摘A microwave mediated solvent free one pot synthesis of formazans is developed using the solid acid, KHSO4. The products were obtained in a short reaction time in high yield. This study was undertaken to find an alternative and green method for the synthesis of formazans in the absence of corrosive mineral acids, buffered solutions and volatile organic compounds (VOCs).
