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A series of 2-methylpropan-2-aminium O-methyl 1-(substituted phenoxyacetoxy)alkylphosphonates (5a-5o) was selectively synthesized by reacting the corresponding O,O-dimethyl l-(substituted phenoxyacetoxy)-alkylphosphonates with an excess of 2-methylpropan-2-amine.The results of preliminary bioassays show that the title compounds exhibit moderate to good herbicidal activities against Brassica napus and Echinochloa crusgalli.Furthermore,compounds 5a-5j,which show much higher activities than compounds 5k-5o,were selected to further evaluate their post-emergence herbicidal activity at a dosage of 150 g/ha(l ha=10000 m2).Especially,2-methylpropan-2-aminium O-methyl 1-[2-(4-chloro-2-methylphenoxy)acetoxy]butylphosphonate(5h) shows 100% inhibitory effect on the growth of Brassica juncea and Amaranthus retroflexus,which is comparable with the commercial herbicide 2,4-dichlorophenoxy acetic acid(2,4-D). 相似文献
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Synthesis of (S)-2-Ethoxy-3-Phenylpropanoic Acid Derivatives and Their Insulin-Sensitizing Activity 总被引:1,自引:0,他引:1
A series of (S)-2-ethoxy-3-phenylpropanoic acid derivatives were synthesized and their insulin-sensitizing activities were evaluated in 3T3-L1 cells. Compounds 1b, 1d, 1e and 1f exhibited more potent insulin-sensitizing activity than rosiglitazone. 相似文献
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Syntheses of 1,3,4-Thia(oxa)diazole-substituted Pyrazole Derivatives and Their Fungicidal Activities
WANGWen-yan ZHAOWei-guang LIZheng-ming 《高等学校化学研究》2004,20(5):543-547
A series of 1,3,4-oxadiazole or 1.3.4-thiadiazole-substituted pyrazole derivatives were synthesized from 4-pyrazole formhydrazide; their biological activities were studied. The structures of all the new compounds were confirmed by means of spectroscopic methods and microanalyses. The preliminary bioassay results indicate that some compounds of them have a good fungicidal activity against Phoma asparagi and Physalospora piricola Nose. 相似文献
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A novel compound N-(4-methylbenzyl)-4-(3-fluorophenyl)-4-piperidinol hydrochloride has been synthesized and its structure (C19H23ClFNO, Mr = 335.83) was characterized by elemental analysis, IR, ^1H NMR, MS and single-crystal X-ray diffraction analyses. The crystal belongs to the triclinic system, space group P1 with a = 7.2163(6), b = 10.7905(9), c = 12.2651(10) A, α = 109.576(2),β = 98.407(2),γ= 95.956(2)°, V= 878.14(13)A3, Z = 2, Dc = 1.270 g/cm^3,μ = 0.231 mm^-1, F(000) = 356, S = 1.100, the final R = 0.0525 and wR = 0.1425 for 3206 unique reflections (Rint = 0.0140) with 2736 observed ones (I 〉 2σ(I)). The piperidine ring exhibits a chair conformation. The dihedral angle made by the methyl- and fluoro-substituted benzene rings is 66.84(7)°. There are some intra- and intermolecular hydrogen bonding interactions among the molecules, which stabilize the whole crystal structure. The preliminary biological activity tests indicate good herbicidal activity for the title compound, in particular against the roots of some tested plants (such as Brassica campestris L. and Echinochloa crusgallis L.). 相似文献
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YAN Lin XUE Si-Jia 《结构化学》2008,27(5):543-546
The new title compound N-(5-(4-chloro-2-(trifluoromethyl)phenyl)furan-2-carbon-yl)- N'-(4,6-dimethylpyrimidin-2-yl)thiourea (C19H14C1F3N4O2S) has been synthesized, and its crystal structure and biological behaviors were studied. The title compound crystallizes in the monoclinic system, space group P21/c with a = 7.932(5), b = 33.46(2), c = 7.556(5) A, β = 98.058(9)°, V = 1986(2) A^3 Mr = 454.85, Z = 4, Dc = 1.521 g/cm^3, μ = 0.349 mm^-1 and F(000) = 928. The structure was solved by direct methods and refined to R = 0.0724 and wR= 0.1429 for 3494 observed reflections (I 〉 2σ(I)). Intermolecular hydrogen bonds along the b axis together with the continuous π-π interactions construct the three-dimensional architecture of the title compound. The preliminary biological tests show definite herbicidalactivity for the title compound. 相似文献
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The γ-substituted β-diketonate 2,4-dioxo-3-pentyl 4-[4-(n-octyloxy)cinnamoyl]oxybenzoate 1 and its pyrazole and isoxazole derivatives (2 and 3 respectively) have been synthesized and characterized by the spectroscopic methods and elemental analysis. The mesogenic properties of these compounds have been studied by polarizing optical microscopy (POM) and differential scanning calorimetry (DSC). A monotropic nematic mesophase was observed for the β-diketonate 1, in contrast, the pyrazole 2 displays an enantiotropic smectic A and isoxazole 3 exhibits an enantiotropic nematic mesophase. The relationship between the structure and liquid crystalline properties has also been discussed. 相似文献
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A novel method for the preparation of chromogenic calixarenes with azo groups was reported.p-Substituted(-NO2,-CH3,-Cl)amilines were diazotized with isoamyl nitrite in EtONa/EtOH under refluxing condition.Fifteen mono-,bis-,tris-and tetrakis(p-substituted phenyl)azo calix[4]arenes (including proximal and distal isomers) were obtainged respectively by diazo-coupling in different molar ratio to calix[4]arenes(1) under pH=7.5-9.0 in non-aqueous solution at 0-5℃.^1H NMR and ^13C NMR spectra of (p-substtituted phenyl)azo calix[4]-arenes indicated that they existed in cone conformation in solution. 相似文献
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Diketo acid derivatives are potent and selective HIV-1 integrase inhibitors. To investigate the detailed synthesis of those derivatives, a series of p/m-[p-(un)substituted phenylsulfonamido]phenyl β-diketo acid derivatives have been designed and synthesized. The quinoxalone derivatives as the potential bioisosteres of the biologically labile β-diketoacid pharmacophores have also been synthesized from reactions of the corresponding diketo acids with o-phenylenediamine. The structures of all diketo acid (ester) and quinoxalone derivatives were confirmed by 1^H NMR, 13^C NMR, IR, HRMS and/or MS (ESI). X-ray crystallographic analysis of 11b demonstrates a similar arrangement of the side chain of quinoxalone derivatives with the parent diketoacids due to the intramolecular hydrogen bond (O…H-N) and the sp^2 hybridization configuration of the two nitrogen atoms of the quinoxalone ring. 相似文献
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Synthesis and Fungicidal Activities of 2-Alkylthio-5- (3, 4, 5-tribenzyloxyphenyl)-1, 3, 4-oxadiazoles 总被引:1,自引:0,他引:1
De Qing LONG De Jiang LI Wei Quan CAI Sheng Sheng CHEN 《中国化学快报》2006,17(11):1427-1430
Abstract: Ten novel 2-alkylthio-5-(3, 4, 5-tribenzyloxyphenyl)-1, 3, 4-oxadiazole derivatives (5a-j) were synthesized from methyl 3, 4, 5-trihydroxybenzoate by ethedfication, hydrazidation, cyclization and thioetherification reactions. The structures of 5a-j were confirmed by 1HNMR, MS spectra and elemental analysis. The results indicated that most of the compounds 5 exhibited good fungicidal activities. The activity of 5h is higher than 90% against Fusarium oxysporum and Botrytis cinereapers in 50 mg/L. 相似文献
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A convenient and efficient method for the highly regioselecfive synthesis of indene derivatives 4 and 5 from tetraaryl substituted 1,3-butadienes 3 was described. The method involves an intramolecular Friedel-Crafts cyclization and a corresponding double-bond positional shift of isomers 4 and 5 in the presence of different Lewis acids under mild conditions with higher than 90% yields. 相似文献
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Qingwu Long Xiaoyan Deng Yujiao Gao Huayong Xie Hao Peng Hongwu He 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):819-825
Abstract A series of sodium hydrogen 1-(substituted phenoxyacetoxy) alkylphosphonates was designed and synthesized. The test for herbicidal activity indicated that most of the phosphonates (8) possessed excellent postemergence herbicidal activities against broadleaf weeds. Especially, 8f and 8g showed the best herbicidal activity against rape and amaranth with more than 95% inhibitory rate. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
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Hao Peng Qingwu Long Xiaoyan Deng Hongwu He 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):1868-1874
Abstract A series of lithium or potassium hydrogen 1-(substituted phenoxyacetoxy)alkylphosphonates were designed and synthesized. All the title compounds were identified by IR, 1H NMR, and 31P NMR, some of them were further analyzed by MS and elemental analyses. The test for herbicidal activity indicated that most of the phosphonates (8) possessed excellent postemergence herbicidal activities against broadleaf weeds. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
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以2,4-二氯嘧啶为起始物设计并合成了一系列4-芳(硫)氧基-2-氯嘧啶和4-芳氧基-2-二甲氨基嘧啶化合物。利用2,4-二氯嘧啶2个氯原子的活性差异,酚取代嘧啶环上4位氯原子,然后二甲氨基取代2位的氯原子。所合成的化合物均经过了1H NMR和元素分析确证。为了确证酚首先在嘧啶环的4位发生亲核取代反应,用X衍射法测定了化合物3d的单晶结构。初步生物活性测定结果表明,大部分化合物都表现出一定的除草活性,其中化合物7c、7j、7k和7m在1.0×10-4g/mL质量浓度下对油菜的抑制率达到了80%以上。 相似文献
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Ling Gao Xiaoyan Deng Xiaosong Tan Qingwu Long Hao Peng Hongwu He 《Phosphorus, sulfur, and silicon and the related elements》2013,188(8):989-994
Abstract A series of 2-methylpropan-2-aminium methyl 1-(substituted phenoxyacetoxy) alkylphosphonates were selectively synthesized by reacting the corresponding dimethyl 1-(substitutedphenoxyacetoxy)alkylphosphonates with an excess of 2-methylpropan-2-amine. All the title compounds were identified by IR, 1H NMR, and 31P NMR, some of them were further analyzed by 19F NMR and 13C NMR. Their herbicidal activity was investigated and the results showed that most of the demethylated aminium salts exhibited notable herbicidal activities against Brassica napus L. and Echinochloa crusgalli. Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfer, and Silicon and the Related Elements for the following free supplemental files: Additional text, figures and tables. 相似文献
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磺酰脲类除草剂是近 2 0年来开发出的超高效、广谱、低毒和高选择性除草剂 .在已研究的磺酰脲分子中 ,芳环的邻位取代基多为酯基、卤素、取代烷氧基、三氟甲基等 [1,2 ] ,而邻位取代基为酰胺基的甚少 .为寻找高活性的磺酰脲化合物 ,本文将活性基团三氟乙酰氨基引入磺酰脲分子中 ,合成了 1 0种 N - (取代嘧啶 - 2 -基 ) - 2 -三氟乙酰氨基苯磺酰脲 (其中 9种为新化合物 ,4b~ 4j) ,并改进了实验方法 ,使产率明显提高 .同时还测定了它们的除草活性 ,其中一些化合物具有良好的活性 .合成路线如下 : X- 4数字显示显微熔点仪 ,温度计未校正… 相似文献
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