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Microwave promoted one-pot synthesis of 3-(2′-amino-3′-cyano-4′-arylpyrid-6′-yl)coumarins 被引量:1
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作者 Jian Feng Zhou Gui Xia Gong +1 位作者 Feng Xia Zhu San Jun Zhi 《Chinese Chemical Letters》 SCIE CAS CSCD 2009年第1期37-39,共3页
A facile procedure for the synthesis of 3-(2′-amino-3′-cyano-4′-arylpyrid-6′-yl) coumarins are being reported starting from 3- acetylcoumarin, aromatic aldehydes and malononitrile. The reactions were carried out... A facile procedure for the synthesis of 3-(2′-amino-3′-cyano-4′-arylpyrid-6′-yl) coumarins are being reported starting from 3- acetylcoumarin, aromatic aldehydes and malononitrile. The reactions were carried out on microwave irradiation in good yield with short time and easy work-up. The structures of all the compounds have been confirmed on the basis of their analytical, IR, ^1H NMR, and mass spectral data. 展开更多
关键词 3-(2′-Amino-3′-cyano-4′arylpyrid-6′-yl) coumarin Aromatic aldehyde 3-Acetylcoumarin Microwave irradiation
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A novel synthesis of 5-aryl-3-cyano-2-pyridones by using vinamidinium salts
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作者 Xue Hui Zhang Wu Zhong Xing Zhou Li Song Li 《Chinese Chemical Letters》 SCIE CAS CSCD 2009年第7期771-774,共4页
A variety of vinamidinium salts were condensated with cyanoacetamide in refluxing methanol that contained sodium methoxide to produce 5-aryl-3-cyano-2-pyridones in good yield. Simple experimental conditions were used ... A variety of vinamidinium salts were condensated with cyanoacetamide in refluxing methanol that contained sodium methoxide to produce 5-aryl-3-cyano-2-pyridones in good yield. Simple experimental conditions were used to prepare ten different 5-aryl-3- cyano-2-pyridones, four of which are new compounds.C 2009 Song Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. 展开更多
关键词 5-Aryl-3-cyano-2-pyridones Vinamidinium salts CYCLIZATION
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SYNTHSIS OF 5-CYANO-2-(4-n-PENTYL-4-BIPHENYLYL)-PYRIMIDINE
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作者 Yong De LI Fang Fang FANG +2 位作者 Lu Ning HAN Qian WANG Dong Hui SHI Chemistry Dept,of Tsinghua University,Beijing 100084 《Chinese Chemical Letters》 SCIE CAS CSCD 1992年第9期699-702,共4页
Condensation of substituted diethyl-malonates with phenylamidine hydrochloride give liquid crystals with a pyrimidine ring,which then subjeet graup transformation to give the title compound—5-cyano-2-(4-n-peatyl-4-bi... Condensation of substituted diethyl-malonates with phenylamidine hydrochloride give liquid crystals with a pyrimidine ring,which then subjeet graup transformation to give the title compound—5-cyano-2-(4-n-peatyl-4-biphenylyl) pyrimidine in high yield. 展开更多
关键词 PYRIMIDINE n-PENTYL-4-BIPHENYLYL SYNTHSIS OF 5-cyano-2
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A Facile Synthesis of 2-Amino-5-Cyano-4, 6-Disubstitutedpyrimidines under MWI
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作者 Kishor S. Jain Swapnil. K. Chaudhari +3 位作者 Nikhil S. More Kapil D. More Sachin A Wakedkar M. K. Kathiravan 《International Journal of Organic Chemistry》 2011年第2期47-52,共6页
Microwave Assisted Organic Synthesis (MAOS) is energy efficient and effective tool to speed up the synthesis for drug discovery process. In the present study we report a novel protocol for the rapid, high throughput s... Microwave Assisted Organic Synthesis (MAOS) is energy efficient and effective tool to speed up the synthesis for drug discovery process. In the present study we report a novel protocol for the rapid, high throughput synthesis of mononuclear 2-amino-5-cyano-4,6-disubstituted pyrimidines, adaptable to parallel synthesis for compound libraries. The overall reaction time in hrs has been reduced to 25 - 50 minutes with improved yields. 展开更多
关键词 Microwave Assisted ORGANIC Synthesis (MAOS) 2-Amino-5-cyano-2 6-Disubstitutedpyrimidines Α-Cyanoketene S S-ACETALS
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Synthesis and Crystal Structure of 1-Methylsulfinyl-1-methylthio-2-cyano-2-phenylethylene
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作者 陈凯 杨华铮 《Chinese Journal of Structural Chemistry》 CSCD 2000年第5期338-342,共5页
The crystal of the title compound (C_ 11H_ 11NOS_2, M_r =237.33) has been prepared and determined by X-ray single crystal diffraction. The crystal is monoclinic, space group P2_1/c with parameters : a=5.484 (1),... The crystal of the title compound (C_ 11H_ 11NOS_2, M_r =237.33) has been prepared and determined by X-ray single crystal diffraction. The crystal is monoclinic, space group P2_1/c with parameters : a=5.484 (1), b=7.793(2), c=28.295(6), β=90.277(4)°, V=1209.2(5)3, Z=4, D_c=1.034 g/cm3, μ(MoKα)= 0.413 mm -1, F(000)=496, the final R=0.0390 and wR=0.1051 for 1500 observed reflections with I>2σ(I). The X-ray analysis result shows that the orientation of methylsulfinyl and phenyl is the cis and confirms the E-stereochemistry of the title compound. 展开更多
关键词 crystal structure SYNTHESIS 1-methylsulfinyl-1-methylthio-2-cyano-2-phenylethylene
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A cesium fluoride promoted efficient and rapid multicomponent synthesis of functionalized 2-amino-3-cyano-4H-pyran and spirooxindole derivatives 被引量:3
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作者 Yogesh B.Wagh Yogesh A.Tayade +3 位作者 Swapnil A.Padvi Bhupesh S.Patil Nilesh B.Patil Dipak S.Dalal 《Chinese Chemical Letters》 SCIE CAS CSCD 2015年第10期1273-1277,共5页
A rapid, one-pot and highly efficient protocol for the synthesis of pharmaceutically interesting functionalized 2-amino-3-cyano-4H-pyran and spirooxindole derivatives has been developed using commercially available Cs... A rapid, one-pot and highly efficient protocol for the synthesis of pharmaceutically interesting functionalized 2-amino-3-cyano-4H-pyran and spirooxindole derivatives has been developed using commercially available Cs F as a catalyst in the reaction of malononitrile and aryl aldehydes or isatins with 1,3-cyclohexanediones. The major advantages of this methodology are excellent yield at ambient temperature, very short reaction time(5–10 min), and use of an inexpensive catalyst. 展开更多
关键词 Cesium fluoride 2-Amino-3-cyano-4H-pyrans Spirooxindoles Rapid synthesis Multicomponent reactions
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New Processes for Annulation
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作者 Liu Hsing-Jang 《合成化学》 CAS CSCD 2004年第z1期18-18,共1页
关键词 annulation 2-cyano-2-cycloalkenones CONJUGATE addition cyclization.
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Metabolic activity of Streptococcus mutans biofilms and gene expression during exposure to xylitol and sucrose 被引量:4
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作者 Eva-Maria Decker Christian Klein +1 位作者 Dimitri Schwindt Christiane von Ohle 《International Journal of Oral Science》 SCIE CAS CSCD 2014年第4期195-204,共10页
The objective of the study was to analyse Streptococcus mutans biofilms grown under different dietary conditions by using multifaceted methodological approaches to gain deeper insight into the cariogenic impact of car... The objective of the study was to analyse Streptococcus mutans biofilms grown under different dietary conditions by using multifaceted methodological approaches to gain deeper insight into the cariogenic impact of carbohydrates. S. mutans biofilms were generated during a period of 24 h in the following media: Schaedler broth as a control medium containing endogenous glucose, Schaedler broth with an additional 5% sucrose, and Schaedler broth supplemented with 1% xylitol. The confocal laser scanning microscopy(CLSM)-based analyses of the microbial vitality, respiratory activity(5-cyano-2,3-ditolyl tetrazolium chloride, CTC) and production of extracellular polysaccharides(EPS) were performed separately in the inner, middle and outer biofilm layers. In addition to the microbiological sample testing, the glucose/sucrose consumption of the biofilm bacteria was quantified, and the expression of glucosyltransferases and other biofilm-associated genes was investigated. Xylitol exposure did not inhibit the viability of S. mutans biofilms, as monitored by the following experimental parameters: culture growth, vitality, CTC activity and EPS production. However,xylitol exposure caused a difference in gene expression compared to the control. Gtf C was upregulated only in the presence of xylitol.Under xylitol exposure, gtf B was upregulated by a factor of 6, while under sucrose exposure, it was upregulated by a factor of three.Compared with glucose and xylitol, sucrose increased cell vitality in all biofilm layers. In all nutrient media, the intrinsic glucose was almost completely consumed by the cells of the S. mutans biofilm within 24 h. After 24 h of biofilm formation, the multiparametric measurements showed that xylitol in the presence of glucose caused predominantly genotypic differences but did not induce metabolic differences compared to the control. Thus, the availability of dietary carbohydrates in either a pure or combined form seems to affect the cariogenic potential of S. mutans biofilms. 展开更多
关键词 biofilms 5-cyano-2 3-ditolyl tetrazolium chloride extracellular polysaccharides gene expression Streptococcus mutans sucrose viability xylitol
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Synthesis and Crystal Structureof Ethyl 5-Amino-1-[(5′-methyl-1′-t-butyl-4′-pyrazolyl)carbonyl]-3-methylthio-1H-pyrazole-4-carboxylate 被引量:1
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作者 李明 文丽荣 +2 位作者 赵桂龙 王啸 杨华铮 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2005年第1期74-78,共5页
The title compound, ethyl 5-amino-1-[(5?-methyl-1?-t-butyl-4?-pyrazolyl)carbonyl] -3-methylthio-1H-pyrazole-4-carboxylate 5, has been synthesized by the treatment of 4 with ethyl 2-cyano-3,3-dimethylthioacryla... The title compound, ethyl 5-amino-1-[(5?-methyl-1?-t-butyl-4?-pyrazolyl)carbonyl] -3-methylthio-1H-pyrazole-4-carboxylate 5, has been synthesized by the treatment of 4 with ethyl 2-cyano-3,3-dimethylthioacrylate, and its crystal structure was determined by X-ray diffraction method. The crystal belongs to monoclinic, space group P21/c with a = 12.194(4), b = 12.909(4), c = 11.607(4) ?, β = 90.183(5)°, V = 1827.2(10) ?3, Mr = 365.45, Z = 4, Dc = 1.328 g/cm3, μ = 0.203 mm-1, F(000) = 776, R = 0.0586 and wR = 0.1558. Preliminary bioassays indicated that the title compound shows fungicidal and plant growth regulation activities. 展开更多
关键词 ethyl 2-cyano-3 3-dimethylthioacrylate PYRAZOLE crystal structure biological activity
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Synthesis of novel benzo[b]pyrimido[4',5':5,4]thieno[2,3-e][1,6]naphthyridine-8-ones via Pictet–Spengler cyclization 被引量:1
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作者 Dao-Lin Wang Xiao-Ce Shi +1 位作者 Yong-Yang Wang Jian Ma 《Chinese Chemical Letters》 SCIE CAS CSCD 2016年第2期261-264,共4页
An efficient method for the synthesis of novel benzo[b]pyrimido[4′,5′:5,4]thieno[2,3e]-[1,6]naphthyridine-8-one derivatives via Pictet-Spengler cyclization is reported. The reaction of 4-(3-aminopyrimido[4,5-d]thi... An efficient method for the synthesis of novel benzo[b]pyrimido[4′,5′:5,4]thieno[2,3e]-[1,6]naphthyridine-8-one derivatives via Pictet-Spengler cyclization is reported. The reaction of 4-(3-aminopyrimido[4,5-d]thieno-2-yl)quinoline-2-ones, which could be obtained from Thorpe-Ziegler isomerization of 4-bromomethylquinoline-2-ones and 5-cyano-1,6-dihydro-4-methyl-2-phenyl-6-thioxopyrimidine,with aromatic aldehydes in the presence of BF3·OEt2 gives pyrimidothieno[1,6]naphthyridines in good yields. 展开更多
关键词 4-Bromomethylquinoline-2-one 5-cyano-6-thioxopyrimidine Pyrimido[4′ 5′:5 4]thieno[2-3e][1 6]naphthyridine Thorpe-Ziegler reaction Pictet-Spengler reaction
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An environmentally friendly synthesis of 1,4-dihydropyrano[2,3-c]pyrazole derivatives catalyzed by tungstate sulfuric acid 被引量:2
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作者 Mahnaz Farahi Bahador Karami +1 位作者 Iman Sedighimehr Hamideh Mohamadi Tanuraghaj 《Chinese Chemical Letters》 SCIE CAS CSCD 2014年第12期1580-1582,共3页
An efficient three-component synthesis of 6-amino-4-aryl-5-cyano-3-metriyl-1-phenyl-1,4-dihydropyrano[2,3-c]pyrazoles via a reaction between 3-methyl-1-phenyl-2-pyrazolin-5-one,aromatic aldehydes and malononitrile usi... An efficient three-component synthesis of 6-amino-4-aryl-5-cyano-3-metriyl-1-phenyl-1,4-dihydropyrano[2,3-c]pyrazoles via a reaction between 3-methyl-1-phenyl-2-pyrazolin-5-one,aromatic aldehydes and malononitrile using tungstate sulfuric acid as a catalyst was described.Mild conditions,good to excellent yields,easily available catalyst and easy work-up are the key features of this method. 展开更多
关键词 6-Amino-4-aryl-5-cyano-3-methyl-1phenyl-1 4-dihydropyrano[2.3-c]pyrazoles 3-Methyl-1-phenyl-2-pyrazolin-5-one Aromatic aldehyde Malononitrile Tungstate sulfuric acid
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Synthesis of 5,6-Diarylpyridin-2(1H)-ones from Isoflavones
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作者 Mulin Zhu Zunting Zhang +3 位作者 Dong Xue Jinfeng Qiao Yong Liang Stanislaw F. Wnuk 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2013年第8期1027-1032,共6页
A simple method for the cyclocondensation of substituted isoflavones with cyanoacetamide in the presence of sodium hydroxide to give an array of 3-cyano-5,6-diarylpyridin-2(1H)-ones in good yields is reported.
关键词 ISOFLAVONES CYCLOCONDENSATION 3-cyano-5 6-diarylpyridin-2(1H)-ones
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Reaction of Ketene Dithioacetals with Pyrazolylcarbohydrazide:Synthesis and Biological Activities of Ethyl 5-Amino-1-(5'- methyl-1'-t-butyl-4'-pyrazolyl)carbonyl-3-methylthio-1H-pyrazole-4-carboxylate
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作者 李明 文丽荣 +3 位作者 付维军 赵桂龙 胡方中 杨华铮 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2004年第9期1064-1066,共3页
The title compound, C16H23N5O3S, ethyl 5-amino-1-(5'-methyl-1'-t-butyl-4'-pyrazolyl)carbonyl-3-methylthio- 1H-pyrazole-4-carboxylate (5) has been synthesized by the treatment of ethyl 2-cyano-3,3-dimethylt... The title compound, C16H23N5O3S, ethyl 5-amino-1-(5'-methyl-1'-t-butyl-4'-pyrazolyl)carbonyl-3-methylthio- 1H-pyrazole-4-carboxylate (5) has been synthesized by the treatment of ethyl 2-cyano-3,3-dimethylthioacrylate with 1-t-butyl-5-methyl-4-hydrazinocarbonylpyrazole (4) in refluxed ethanol. The possible mechanism of the above reaction was also discussed. The results of biological test show that the title compound has fungicidal and plant growth regulation activities. 展开更多
关键词 PYRAZOLE ethyl 2-cyano-3 3-dimethylthioacrylate reaction mechanism biological activity
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Quantitative structure-retention relationship for photosystem Ⅱ inhibitors in RP-HPLC
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作者 王琴孙 张玲 +1 位作者 杨华铮 刘华银 《Chinese Journal of Chemistry》 SCIE CAS CSCD 1998年第6期514-520,共7页
Using factor analysis (principle component) and multiple linear regression methods,4 solute-related structure parameters were selected from 10 structure parameters and the relationships between the retention propertie... Using factor analysis (principle component) and multiple linear regression methods,4 solute-related structure parameters were selected from 10 structure parameters and the relationships between the retention properties (logk’) of 25 2-cyano-3-methylthio-3-substituted amino-acrylates and the 4 parameters were established.There is a good agreement between the observed k’ values and the predicted fe’ values. 展开更多
关键词 2-cyano-3-methylthio-3-substituted amino-acrylates reversed phase HPLC photo-system inhibitors QSRR
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