A one-pot, four-component reaction of ethyl acetoacetate, hydrazine hydrate, aldehydes, and malononitrile was discussed using Lewis acid catalyst morpholine triflate （MorT） to afford a series of dihydropyrano[2,3-c]...A one-pot, four-component reaction of ethyl acetoacetate, hydrazine hydrate, aldehydes, and malononitrile was discussed using Lewis acid catalyst morpholine triflate （MorT） to afford a series of dihydropyrano[2,3-c]pyrazoles, which were generally catalyzed by organic alkalis. Moderate to excellent yields, no chromatographic purification, and evasion of environmentally hazardous solvents in the reaction process make this protocol very useful for academia and industry.展开更多
Iodine catalyzed one-pot reactions of salicylaldehyde and dimolecular 1H-indene-l,3（2H）-dione, barbituric acids, 4-hydro- xycoumarin, or 4-hydroxy-6-methylpyran-2-one were performed and provided a rapid, convenient ...Iodine catalyzed one-pot reactions of salicylaldehyde and dimolecular 1H-indene-l,3（2H）-dione, barbituric acids, 4-hydro- xycoumarin, or 4-hydroxy-6-methylpyran-2-one were performed and provided a rapid, convenient and general approach to synthesize the chromene derivatives. 2-（11-Oxo-10,11-dihydroindeno[1,2-b]chromen-10-yl）-lH-indene-1,3（2H）-diones P1-P4 and 10-（4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl）-3-methylpyrano[4,3-b]chromen-1（1OH）-ones P8-P9 were unprecedentedly prepared and structurally identified by NMR and Mass. The confirmation of structure by single crystal X-ray crystallography is reported for P3.展开更多
The title compound （C19H17BrN2O4） was synthesized via a one-pot procedure starting from 4-bromobenzaldehyde, dimethyl acetylenedicarboxylate （DMAD） and phenylhydrazine with pyridine as the catalyst. Its structure ...The title compound （C19H17BrN2O4） was synthesized via a one-pot procedure starting from 4-bromobenzaldehyde, dimethyl acetylenedicarboxylate （DMAD） and phenylhydrazine with pyridine as the catalyst. Its structure was determined by single-crystal X-ray diffraction analysis. The crystal belongs to the monoclinic system, space group P21/c with a = 11.115（3）, b = 8.090（2）, c = 20.211（5） , β = 97.032（5）°, V = 1803.7（8） 3, Z = 4, Mr = 417.25, Dc = 1.536 g/cm3, μ = 2.306 mm-1, F（000） = 852, the final R = 0.0403 and wR = 0.0895 for 2215 observed reflections with I 2σ（I）.展开更多
The title compound （C26H20ClN3O3） has been synthesized by 1,3-dipolar cycloaddition reaction from isatin, sarcosine and （Z）-4-（4-chlorobenzylidene）-2-phenyloxazol-5（4H）-one through a one-pot procedure, and its...The title compound （C26H20ClN3O3） has been synthesized by 1,3-dipolar cycloaddition reaction from isatin, sarcosine and （Z）-4-（4-chlorobenzylidene）-2-phenyloxazol-5（4H）-one through a one-pot procedure, and its structure was confirmed by IR, IH NMR, elemental analysis and single-crystal X-ray diffraction analysis. The crystal belongs to the triclinic system, space group PI, with a = 9.3903（19）, b = 11.398（2）, c = 12.603（3） A, α = 83.495（3）, β = 68.988（3）, γ = 67.178（3）^o, V= 1160.1（4）A^3 Z = 2, Mr= 457.90, Dc= 1.311 g/cm^3, p = 0.198 mm ^-1, F（000） = 476, the final R = 0.0489 and wR = 0.1144 for 3109 observed reflections with I 〉 2σ（I）.展开更多
The title compound （C30H27NO3） was synthesized via a one-pot procedure starting from fl-benzoylthioacetanilide, benzaldehyde and 5,5-dimethyl-1,3-cyclohexanedione, and its structure was determined by single-crystal ...The title compound （C30H27NO3） was synthesized via a one-pot procedure starting from fl-benzoylthioacetanilide, benzaldehyde and 5,5-dimethyl-1,3-cyclohexanedione, and its structure was determined by single-crystal X-ray diffraction analysis. The crystal belongs to triclinic system, space group PI, with a = 6.325（2）, b = 11.243（3）, c = 17.553（4） A, a = 87.306（4）, β = 80.822（4）, γ = 77.798（4）°, V= 1204.2（5） A^3, Z = 2, Mr= 449.53, Dc= 1.240 g/cm^3, p = 0.080 mm^-1, F（000） = 476, the final R = 0.0459 and wR = 0.0970 for 2301 observed reflections with I 〉 2σ（I）.展开更多
The title compound （C22H22N2O2Fe·CH3OH） was synthesized via a one-pot procedure from ferrocenylaldehyde, malononitrile and 5,5-dimethyl-1,3-cyclohexanedione using room temperature ionic liquid and pyridine as t...The title compound （C22H22N2O2Fe·CH3OH） was synthesized via a one-pot procedure from ferrocenylaldehyde, malononitrile and 5,5-dimethyl-1,3-cyclohexanedione using room temperature ionic liquid and pyridine as the catalysts, and characterized by elemental analysis, IR and ^1H NMR. The structure was determined by X-ray single-crystal diffraction. The crystal belongs to monoclinic system, space group P21/n, with a = 9.7085（15）, b = 22.951（4）, c = 9.987（2） A, β = 112.494（3）°, V = 2055.9（6）A^3 Z = 4, Mr= 402.28, De= 1.403 g/cm^3, p = 0.759 mm^-1, F（000） = 868, the final R = 0.0536 and wR = 0.1449 for 4202 observed reflections with I 〉 2σ（I）. The supramolecular single-helix chain of the title compound is formed by linking the building units with the hydrogen bond between N1 and N2. The adjacent chains are connected to a 2D layer by the hydrogen bond between N1 and O1. The adjacent layers are further linked by van der waals＇ force. The CH3OH molecule is trapped in the interlayer.展开更多
A series of compounds containing the 1H-pyrazino[1,2-a]quinoxaline-1,5(6H)-dione scaffold have been synthesized using a one-pot procedure under microwave irradiation. This new strategy allowed for the facile synthesis...A series of compounds containing the 1H-pyrazino[1,2-a]quinoxaline-1,5(6H)-dione scaffold have been synthesized using a one-pot procedure under microwave irradiation. This new strategy allowed for the facile synthesis of target compounds in good yields and could be readily applied to the construction of diverse libraries of compounds for high throughput screening in medicinal chemistry.展开更多
The convenient and efficient procedure for one-pot preparation of quinaldine derivatives from multi component reaction of anilines, acetone and benzaldehyde without any solvent under microwave irradiation on the surfa...The convenient and efficient procedure for one-pot preparation of quinaldine derivatives from multi component reaction of anilines, acetone and benzaldehyde without any solvent under microwave irradiation on the surface of alumina impregnated with hydrochloric acid is developed.展开更多
An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydr...An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.展开更多
Caffeine was applied as a green and natural catalyst for the one-pot,four-component sequential condensation between 2-hydroxy-1,4-naphthoquinone,aromatic 1,2-diamines,ammonium thiocyanate and acid chlorides in the pre...Caffeine was applied as a green and natural catalyst for the one-pot,four-component sequential condensation between 2-hydroxy-1,4-naphthoquinone,aromatic 1,2-diamines,ammonium thiocyanate and acid chlorides in the presence of a basic ionic liquid（l-butyl-3-methylimidazolium hydroxide） to afford the corresponding benzo[a][1,3]oxazino[6,5-c]phenazine derivatives.In this one-pot transformation,five bonds and two new rings are efficiently formed.This protocol has the advantages of operational simplicity,high yields,easy workup,avoidance of hazardous or toxic catalysts and organic solvents and high chemo-and regioselectivities.展开更多
文摘A one-pot, four-component reaction of ethyl acetoacetate, hydrazine hydrate, aldehydes, and malononitrile was discussed using Lewis acid catalyst morpholine triflate （MorT） to afford a series of dihydropyrano[2,3-c]pyrazoles, which were generally catalyzed by organic alkalis. Moderate to excellent yields, no chromatographic purification, and evasion of environmentally hazardous solvents in the reaction process make this protocol very useful for academia and industry.
文摘Iodine catalyzed one-pot reactions of salicylaldehyde and dimolecular 1H-indene-l,3（2H）-dione, barbituric acids, 4-hydro- xycoumarin, or 4-hydroxy-6-methylpyran-2-one were performed and provided a rapid, convenient and general approach to synthesize the chromene derivatives. 2-（11-Oxo-10,11-dihydroindeno[1,2-b]chromen-10-yl）-lH-indene-1,3（2H）-diones P1-P4 and 10-（4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl）-3-methylpyrano[4,3-b]chromen-1（1OH）-ones P8-P9 were unprecedentedly prepared and structurally identified by NMR and Mass. The confirmation of structure by single crystal X-ray crystallography is reported for P3.
基金Supported by the National Natural Science Foundation of China (No. 20872074)Natural Science Foundation of Shandong Province (Y2006B11 and Z2008B03)
文摘The title compound （C19H17BrN2O4） was synthesized via a one-pot procedure starting from 4-bromobenzaldehyde, dimethyl acetylenedicarboxylate （DMAD） and phenylhydrazine with pyridine as the catalyst. Its structure was determined by single-crystal X-ray diffraction analysis. The crystal belongs to the monoclinic system, space group P21/c with a = 11.115（3）, b = 8.090（2）, c = 20.211（5） , β = 97.032（5）°, V = 1803.7（8） 3, Z = 4, Mr = 417.25, Dc = 1.536 g/cm3, μ = 2.306 mm-1, F（000） = 852, the final R = 0.0403 and wR = 0.0895 for 2215 observed reflections with I 2σ（I）.
基金Supported by the National Natural Science Foundation of China (No. 20572057)Natural Science Foundation of Shandong Province (Y2006B11)
文摘The title compound （C26H20ClN3O3） has been synthesized by 1,3-dipolar cycloaddition reaction from isatin, sarcosine and （Z）-4-（4-chlorobenzylidene）-2-phenyloxazol-5（4H）-one through a one-pot procedure, and its structure was confirmed by IR, IH NMR, elemental analysis and single-crystal X-ray diffraction analysis. The crystal belongs to the triclinic system, space group PI, with a = 9.3903（19）, b = 11.398（2）, c = 12.603（3） A, α = 83.495（3）, β = 68.988（3）, γ = 67.178（3）^o, V= 1160.1（4）A^3 Z = 2, Mr= 457.90, Dc= 1.311 g/cm^3, p = 0.198 mm ^-1, F（000） = 476, the final R = 0.0489 and wR = 0.1144 for 3109 observed reflections with I 〉 2σ（I）.
基金This project was supported by the N N S Foundation of China (No. 20572057) N S Foundation of Shandong province (Y2006B11)
文摘The title compound （C30H27NO3） was synthesized via a one-pot procedure starting from fl-benzoylthioacetanilide, benzaldehyde and 5,5-dimethyl-1,3-cyclohexanedione, and its structure was determined by single-crystal X-ray diffraction analysis. The crystal belongs to triclinic system, space group PI, with a = 6.325（2）, b = 11.243（3）, c = 17.553（4） A, a = 87.306（4）, β = 80.822（4）, γ = 77.798（4）°, V= 1204.2（5） A^3, Z = 2, Mr= 449.53, Dc= 1.240 g/cm^3, p = 0.080 mm^-1, F（000） = 476, the final R = 0.0459 and wR = 0.0970 for 2301 observed reflections with I 〉 2σ（I）.
基金the National Natural Science Foundation of China (No. 20572057) Natural Science Foundation of Shandong Province (Y2006B11)
文摘The title compound （C22H22N2O2Fe·CH3OH） was synthesized via a one-pot procedure from ferrocenylaldehyde, malononitrile and 5,5-dimethyl-1,3-cyclohexanedione using room temperature ionic liquid and pyridine as the catalysts, and characterized by elemental analysis, IR and ^1H NMR. The structure was determined by X-ray single-crystal diffraction. The crystal belongs to monoclinic system, space group P21/n, with a = 9.7085（15）, b = 22.951（4）, c = 9.987（2） A, β = 112.494（3）°, V = 2055.9（6）A^3 Z = 4, Mr= 402.28, De= 1.403 g/cm^3, p = 0.759 mm^-1, F（000） = 868, the final R = 0.0536 and wR = 0.1449 for 4202 observed reflections with I 〉 2σ（I）. The supramolecular single-helix chain of the title compound is formed by linking the building units with the hydrogen bond between N1 and N2. The adjacent chains are connected to a 2D layer by the hydrogen bond between N1 and O1. The adjacent layers are further linked by van der waals＇ force. The CH3OH molecule is trapped in the interlayer.
基金supported by the Scientific Research Foundation of Chongqing University of Arts and Sciences(R2013XY01,R2013XY02)the Chongqing Science and Technology Commission(CSTC2013JCYJA50028)SRF for ROCS,SEM
文摘A series of compounds containing the 1H-pyrazino[1,2-a]quinoxaline-1,5(6H)-dione scaffold have been synthesized using a one-pot procedure under microwave irradiation. This new strategy allowed for the facile synthesis of target compounds in good yields and could be readily applied to the construction of diverse libraries of compounds for high throughput screening in medicinal chemistry.
文摘The convenient and efficient procedure for one-pot preparation of quinaldine derivatives from multi component reaction of anilines, acetone and benzaldehyde without any solvent under microwave irradiation on the surface of alumina impregnated with hydrochloric acid is developed.
基金supported by Special Assistance Programme SAP,University Grants Commission,New Delhi,India
文摘An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.
基金financial support from the Research Council of Young Researchers and Elite Club,Yazd Branch,Islamic Azad University,Yazd,Iran and University of Science and Arts of Yazd,Iran
文摘Caffeine was applied as a green and natural catalyst for the one-pot,four-component sequential condensation between 2-hydroxy-1,4-naphthoquinone,aromatic 1,2-diamines,ammonium thiocyanate and acid chlorides in the presence of a basic ionic liquid（l-butyl-3-methylimidazolium hydroxide） to afford the corresponding benzo[a][1,3]oxazino[6,5-c]phenazine derivatives.In this one-pot transformation,five bonds and two new rings are efficiently formed.This protocol has the advantages of operational simplicity,high yields,easy workup,avoidance of hazardous or toxic catalysts and organic solvents and high chemo-and regioselectivities.
