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1.
1 INTRODUCTION The pyrazolo[1,5-a]pyrimidines are the active compositions in many pesticides and medicines. A new class of KDR (tyrosine kinase VEGFR-2) ki- nase inhibitors is discovered and found to have affi- nity for the human CRF-1 (Corticotrophin re…  相似文献   

2.
The title compound was prepared by reaction of N, N‐dimethyldithiocarbamate sodium with l‐bromo‐l‐(4‐methoxyphenylcarbonyl)‐2‐(1, 2, 4‐triazole‐l‐yl) ethane. Its crystal structure has been determined by X‐ray diffraction analysis. The crystal belongs to triclinic with space group Pī, a = 0.7339(2) nm, b = 1.1032(2) nm, c = 1.1203(2) nm, a = 90.27(3)°, β = 102.03(3)°, γ = 104.91(3)°, Z=2, V = 0.8556(3) nm3, Dc = 1.360 g/cm3, μ =0.325 mm?1, F(000)=368, final R1 =0.0475. The planes of 4‐methoxybenzyl group and triazole ring are nearly perpendicular to each other. The dihedral angle is 83.97°. There is an obvious π‐π stacking interaction between the molecules in the crystal lattice. The results of biological test show that the title compound has fungicidal and plant growth regulating activities.  相似文献   

3.
1INTRODUCTIONThepyrazolo[3,4-b]pyridineclassofcompoundspossessmanybiologicalandpharmacologicalactivi-ties[1],suchasactiveanti-concretionmedicaments[2]aswellasactiveanti-gramnegativeandpositivebacteriaagents[3].Thereforethesynthesesofsuchcompoundshavearousedgreatattentionofalargenumberofchemists.Themostimportantsyntheticrouteisthecondensationreaction[4~11]ofamino-pyrazoleandα,β-unsaturatedcompounds.Theorganicreactionundermicrowaveirradia-tionhastheadvantagesoffastreactionspeed,shorttime…  相似文献   

4.
On the basis of the Zaleplon structure, novel pyrazolo[1,5-a]pyrimidines were designed and prepared for studies on their hypnotic activity. This paper reported the synthesis of twelve new 5-methyl-7-substituted-pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives by using simple starting materials such as propane dinitrile and triethyl orthoformate. The structures of the derived target compounds were confirmed by their IR and ^1H-NMR spectroscopic data. The preliminary pharmacological evaluations indicated that some compounds showed hypnotic activity, whilc derivative 1c was the most potent one.  相似文献   

5.
6.
1 INTRODUCTION The acyl ureas are a kind of high biological acti- vity compounds with low toxicity to mammals, birds, fish, amphibians, etc., and significant organic synthe- sis intermediates working extensively as insecticides, pesticides, fungicides and herbicides in agrochemi- cal industry[1~7]. While pyrimidinyl derivatives show excellent biological activities in the development of pesticide, and are used to develop high effective and high select herbicides. For example, pyrimidiny su…  相似文献   

7.
The title compound, 2-(methoxybenzoyl)-N-phenyl-2-(1,2,4-triazol-l-yl) thioacetamide was synthesized by several reactions from 4-methoxyacetophenone, triazole and phenyl isothiocyanate. The structure was identified by elemental analysis, ^1H NMR, MS and IR. The single crystal structure of 2-(methoxybenzoyl)-N-phenyl-2-(1,2,4-triazol-l-yl)thioacetamide was determined withX-ray diffraction. The preliminary bioassays show that the title compound exhibits weak antifungal activities and plant-growth regulatory activity.  相似文献   

8.
The title compound (C20H21N3O4, Mr = 367.40) has been synthesized and its crystal structure was determined by single-crystal X-ray diffraction. The crystal is of orthorhombic, space group P212121 with a = 7.5143(15), b = 13.901(3), c = 18.545(4) , V = 1937.1(7) 3, Z = 4, Dc = 1.260 g/cm3, μ = 0.089 mm-1, F(000) = 776, the final R = 0.0616 and wR = 0.0912. X-ray diffraction reveals that the molecule adopts an E configuration about the central C=N double bond. The intermolecular O–H…O hydrogen bond stabilizes the crystal structure by causing the formation of a supramolecular architecture.  相似文献   

9.
1 INTRODUCTION Recently, compounds containing pyrazole, imida- zole, triazole (including benzotriazole), pyridine, tetrazole and indole have attracted much interest because of their fungicidal activity, plant-growth regulating activity and antibacterial activity[1~3]. Schiff bases also constitute a good type of biolo- gically active substructures[4~7]. Studies of pyri- dine Schiff base-type fungicides have been repor- ted[8]. However, some structures of pyridine com- pounds containing h…  相似文献   

10.
6,8-Dimethoxy-3-[2-(4-methoxyphenyl)ethyl]isocoumarin was synthesized by condensation of 5,7-dimethoxyhompophthalic acid with 3-(4-methoxyphenyl)propanoyl chloride. The structure of the synthesized compound was confirmed by its mass spectrometric studies. The synthesized compound serves as a model for synthesis of DL-agrimonolide.  相似文献   

11.
The crystal structure of ethyl 2-methylthio-7-phenylpyrazolo[l,5-a]pyrimidine-3- carboxylate (C16H15N3O2S, Mr = 313.37) has been determined by single-crystal X-ray diffraction analysis. The crystal belongs to monoclinic, space group P21/n with a = 19.361(7), b = 7.595(3), c = 20.910(8) (A), β = 94.925(6)°, V= 3064(2) (A)3, Z = 8, Dc= 1.359 g/cm3,μ = 0.222 mm-1, F(000) = 1312, R = 0.0546 and wR = 0.1082 for 5374 unique reflections with 3419 observed ones (I > 2σ(I)). The results show that all ring atoms in the pyrazolopyrimidine moiety are coplanar with strong tensile force. The structure analysis indicates that the single crystal contains strong nonclassical hydrogen bonds.  相似文献   

12.
The title compound, C16H14N4S, has been synthesized by the reaction of pentane-2,4-dione with 5-amino-3-benzylthio-4-cyano-l-H-pyrazole in ethanol, and its crystal structure was determined by X-ray diffraction method. The crystal is of monoclinic, space group P21/n with a=8.699(3), b=23.139(9), c=7.536(3) A, β= 92.400(8)°, V= 1515.5(10) A3, Z=4,Mr=294037, Dc= 1.290 g/cm3, λ=0.71073 A,μ(MoKo)=0.212 mm-1 and F(000)=616. The structure was refined to R=0.0533 and wR=0.1141 for 2672 unique reflections with Rint= 0.06.distance of 3.875 A and the angle of 164.8°.  相似文献   

13.
14.
李明  郭维斯  文丽荣  杨华铮 《有机化学》2005,25(10):1230-1234
利用取代烯胺酮1与3-甲硫基-4-氰基-5-氨基-1H-吡唑(2)反应,用传统和微波2种方法合成了6种化合物2-甲硫基-3-氰基-7-取代苯基吡唑并[1,5-a]嘧啶(3a~3f),化合物的结构均经元素分析,IR,1H NMR所证实.对比两种方法,微波辐射具有用时少、环境友好、易纯化和产率高的特点,同时,探讨了反应可能的机理,并对所有化合物的杀菌和除草活性进行了测试.  相似文献   

15.
The crystal structure of the title compound has been determined by single crystal X-ray diffraction analysis. C15H14N4O3, Mr=298.30, monoclinic, space group P21/n, a=9.483(9),b=11.078(9), c=13.700(9),β=100.19(7)°, V=1417(4)3, Z=4, Dx=1.399 g.cm-3, μ=0.0942 mm-1; F(000)=624, final R=0.074 and Rw=0.074 for 1502 observed reflections[I≥3σ(I)]. The results show that all ring atoms in the triazolopyrimidinyl moiety were coplanar with strong tensile force, which might be an important active site.  相似文献   

16.
以乙氧基甲叉基氰乙酸乙酯和对氟苯乙酮为起始原料,设计并合成了新化合物5-(4-氟苯基)-N-1-(3-羟基金刚烷基)-7-三氟甲基吡唑并[1,5-a]嘧啶-3-酰胺(7),其结构经~1H NMR,IR和HR-MS(ESI)表征。采用MTT法测定了其对人乳腺癌细胞(Bcap-37)、人宫颈癌细胞(He La229)、人肝癌细胞(QGY-7701)和人肺癌细胞(A549)体外抗肿瘤细胞的增殖活性。结果表明:7对受试细胞的抑制活性较好,其IC_(50)值分别为23.9μmol·L~(-1),29.8μmol·L~(-1),31.4μmol·L~(-1)和21.7μmol·L~(-1)。  相似文献   

17.
王胜  冯桂荣  刘国华  叶文法  汪焱钢 《有机化学》2006,26(11):1584-1586
通过2-氨基-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶同芳酰基异硫氰酸酯反应, 合成了12种新的含杂环基的芳酰基硫脲, 用红外光谱、核磁共振氢谱和元素分析确证了其结构, 初步的生物活性测定试验表明部分目标化合物具有良好的生物活性, 尤其是对于双子叶植物表现出较高的除草活性.  相似文献   

18.
马忠华  刘祖明  陈琼 《有机化学》2008,28(11):1965-1970
以2-巯基-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶为原料, 设计合成了17种含5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶环和1,2,4-三唑环的新型双杂环化合物, 结构经元素分析, MS, 1H NMR及13C NMR进行表征. 初步的生物活性测试表明, 部分化合物表现出较好的杀菌、除草活性.  相似文献   

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