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1.
合成了4个2-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-基硫代]-1-(2,3,4-三甲氧)苯乙酮肟醚新化合物, 并经过元素分析、红外光谱、核磁共振氢谱对其结构进行了表征. 初步生物活性测试表明, 化合物具有一定抗烟草花叶病毒活性.  相似文献   

2.
以3,3-二甲基-1-(1H-1,2,4-三唑基)-2-丁酮肟为原料,经醚化、肼解及腙化3步反应得到(E)-N'-(取代苯亚甲基)-2-[(Z)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)丁基-2-亚甲氨氧基]乙酰肼(3a~3u),化合物3与二乙酸碘苯(IBD)反应,合成了21个(Z)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)-2-丁酮肟-(5-芳基-1,3,4-噁二唑-2-基)甲基醚(4a~4u),化合物4的化学结构经核磁共振谱、高分辨质谱和元素分析确证.采用单晶X射线衍射仪测定了化合物4c的晶体结构.抑菌活性测试结果表明,在500 mg/L浓度下,化合物4k,4f,4j和4n对纹枯病菌的防效率分别为70.9%,60.2%,60.0%和60.6%;在25 mg/L浓度下,化合物4b,4c,4d和4e对菌核病菌的抑制率为71.8%~76.9%.  相似文献   

3.
采用中间体衍生化方法, 以环唑醇中间体1-(4-氯苯基)-2-环丙基丙酮作为基本骨架, 引入肟醚活性片段, 合成了32个新的1-(4-氯苯基)-2-环丙基酮肟醚类化合物, 其化学结构经核磁共振波谱和质谱等确认. 单晶X衍射分析表明, 化合物2n属于单斜晶系, 空间群为P21/c. 生物活性筛选结果表明, 化合物1i在200 mg/L浓度下对蚜虫的致死率为78.57%; 化合物1g在200 mg/L浓度下对红蜘蛛的致死率为69.95%; 化合物1i在200和12.5 mg/L浓度下对黏虫的致死率分别为100%和85%.  相似文献   

4.
以3-甲基吡啶、特戊酸乙酯、盐酸羟胺和取代苯甲酸等为原料,经加成、肟化和酯化反应,合成了12种新型的3,3-二甲基(吡啶-3-基)-丁-2-酮肟酯.该方法反应条件比较温和、收率高.化合物的结构通过IR、~1H NMR、~(13)C NMR和元素分析确证.采用菌丝生长速率法测试了目标化合物对两种病原菌的离体抑制活性,O-(4-溴苯甲酰基)-3,3-二甲基-1-(吡啶-3-基)-丁-2-酮肟(3h)和O-(4-氯苯甲酰基)-3,3-二甲基-1-(吡啶-3-基)-丁-2-酮肟(3j)对菌核菌有较强的抑制活性,EC50值分别为5.07和4.81μg/mL;3h、3j和O-(3,4-二氯苯甲酰基)-3,3-二甲基-1-(吡啶-3-基)-丁-2-酮肟(3l)对灰霉菌显示出较高的抑制活性,EC50值分别为4.98、5.44和6.34μg/mL.  相似文献   

5.
以间二氯苯、氯乙酰氯和咪唑为原料 ,利用成肟和引入咪唑基顺序不同 ,首先合成了 E-,Z-2 -(1 -咪唑基 ) -2 ,4 -二氯苯乙酮肟 ( E、IZ) ,从二氯苯合成了 α-氯 -二氯取代乙苯 ( A、 B和 C) ,咪唑基 -二氯苯乙酮肟顺反异构体 ( Z、 E)分别与 α-氯 -二氯乙苯反应 ,生成 E-、Z-2 -(1 -咪唑基 ) -O-(α-甲基 -二氯苄基 ) -2 ,4 -二氯苯乙酮肟硝酸盐共 6种新化合物 ,产率为 5 7.5 %~ 64 .5 %,新化合物结构经元素分析、IR和 1H NMR表征 .初步实验表明 ,各化合物对水稻苗腐根有不同程度抑制活性 .  相似文献   

6.
曹世民  刘启旺  田福利 《化学学报》1996,54(11):1132-1137
用苯甲酰(或溴代苯甲酰)二茂铁肟与丙烯腈进行氰乙基化反应, 得到三种新的二茂铁衍生物(含一种肟)。对它们进行了元素分析、IR、^1H NMR谱表征, 并测定了两种化合物的分子和晶体结构。  相似文献   

7.
以焦脱镁叶绿酸-α甲酯为起始原料并转化成(E/Z)-焦脱镁叶绿酸-131-酮肟,经历与NCS的亲电取代、硝酸铊或四氧化锇的氧化以及与重氮甲烷的1,3-偶极环加成等不同化学反应,生成了一系列二氢卟吩化合物.新合成的叶绿素衍生物的化学结构均经紫外-可见光谱、红外光谱、核磁共振光谱和元素分析予以确认.  相似文献   

8.
以雄甾-4-烯-3,17-二酮(AD)为起始原料,合成了14个甾体17位肟醚和肟酯类新化合物.所合成的化合物结构均经过MS,1H NMR谱确证,并对所合成的化合物进行了老鼠5α-还原酶抑制生物活性初步评价.结果表明:受试化合物均有一定的5α-还原酶抑制活性,其中化合物5a,5c,5d有较高的5α-还原酶抑制活性,与参比药物Espristeride相当.  相似文献   

9.
新型5-芳基-N-吡唑肟酯化合物的合成与杀菌活性   总被引:4,自引:1,他引:3  
以水杨醛和丙酮缩合形成α,β不饱和酮,与水合肼和冰乙酸关环形成5-(2-羟基苯基)吡唑酮骨架,合成了10种未见报道的1-(5-(2-(苯氧基)苯基)-3-甲基)-4,5-二氢-N-吡唑肟酯类衍生物.通过元素分析、红外光谱及核磁共振氢谱测试技术对其结构进行了表征,初步测定了化合物的杀菌活性.结果表明,化合物对小麦赤霉病菌有较好的杀灭活性(其中化合物5f杀灭活性达到81.3%);化合物5g和5i对水稻纹枯病菌有中等杀灭活性,对稻瘟病菌的杀灭活性差.成了10种未见报道的1-(5-(2-(苯氧基)苯基)-3-甲基)-4,5-二氢-N-吡唑肟酯类衍生物.通过元素分析、红外光谱及核磁共振氢谱测试技术对其结构进行了表征,初步测定了化合物的杀菌活性.结果表明,化合物对小麦赤霉病菌有较好的杀灭活性(其中化合物5f杀灭活性达到81.3%);化合物5g和5i对水稻纹枯病菌有中等杀灭活性,对稻瘟病菌的杀灭活性差.  相似文献   

10.
以雄甾-4-烯-3,17-二酮(AD)为起始原料, 合成了14个甾体17位肟醚和肟酯类新化合物. 所合成的化合物结构均经过MS, 1H NMR谱确证, 并对所合成的化合物进行了老鼠5α-还原酶抑制生物活性初步评价. 结果表明: 受试化合物均有一定的5α-还原酶抑制活性, 其中化合物5a, 5c, 5d有较高的5α-还原酶抑制活性, 与参比药物Espristeride相当.  相似文献   

11.
We describe the synthesis and characterization of two new zinc (II) and cadmium (II) complexes of the tetradentate dissymmetric Schiff base ligand 2-((E)-(2-(2-(pyridine-2-yl)ethylthio)ethylimino)methyl)-4-bromophenol (PytBrsalH), prepared from 1-(2-pyridyl)-3-thia-5-aminopentane (pyta) and 5-bromosalicylaldehyde. The complexes were synthesized by treating an ethanolic solution of the ligand with equimolar amounts of appropriate metal salts in 1 M methanolic solution of NaOH or alternatively, by a more direct route in which the two reactants are added to a solution of the ligand immediately after formation of the latter and prior to any isolation. The complexes were characterized by elemental analysis, FTIR, (1)H-NMR, electronic spectra and molar conductivity. According to obtained data, the probable coordination geometries of zinc and cadmium in these complexes with mixed N, S and O donor atoms are tetrahedral- and octahedral-like,respectively. Both complexes were found to be 1:1 electrolyte systems in acetonitrile.  相似文献   

12.
A new sulfonyl group-containing heterocyclic compound 2-(2-chloro-4-nitrophenylsulfonyl)-1-(2-thienyl)ethanone 2 was prepared from the corresponding sulfide 2-(2-chloro-4-nitrophenylthio)-1-(2-thienyl)ethanone 1 . Two different cyclization reactions of the compound 2 were discussed. In contrast to the tandem alkylation-cyclization process [1], another cyclic procedure was described. In the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene as a base and dimethylformamide as a solvent, compound 2 was treated with ethyl acrylate or methyl methacrylate at 50–55° to give the 1,4-benzoxathiin 4,4-dioxide 5 or 6 respectively via a tandem Michael conjugate addition-cyclization process.  相似文献   

13.
The reaction of a new antitumor platinum complex, (R)-(-)-2-aminomethylpyrrolidine(1,1-cyclobutanedicarboxylato++ +)platinum(II) (1) with guanosine at room temperature in an aqueous solution was followed by proton nuclear magnetic resonance (1H-NMR) spectroscopy and high performance liquid chromatography (HPLC) at intervals. Both techniques showed that a new compound was formed by displacement of the 1,1-cyclobutanedicarboxylate moiety of 1 with two guanosines, and its 1H-NMR spectrum and HPLC chromatogram were proved to be identical with those of [(R)-(-)-2-aminomethylpyrrolidine]bis(N7-guanosine)platinum(II) (2), which was obtained upon successive treatment of (R)-(-)-2-aminomethylpyrrolidinedichloroplatinum(II) (3) with AgNO3 and 2 mol eq of guanosine in water. The binding sites of the platinum to the two guanosine moieties in 2 were confirmed by the pH dependence of the two G-H8 signals.  相似文献   

14.
用中压汞灯(λ > 300 nm)照射4-苯乙烯基吡啶、2-苯乙烯基苯并噁唑和5-苯基-2-苯乙烯基噁唑三种杂芳基乙烯单体中任意两种的硫酸水溶液,得到三种交叉二聚体.用高效液相色谱跟踪研究了交叉光二聚反应,发现每组反应生成三种光二聚体,其中二种为单体自身的光二聚体,而另外一种是两种不同单体的交叉光二聚体.交叉二聚体通过柱色谱分离得到,其顺式头对尾结构经紫外、红外、氢谱、碳谱和元素分析确定.用紫外光谱和高效液相色谱跟踪研究了交叉光二聚体的稀溶液在低压汞灯(λmax=254 nm)照射下的光解反应.研究发现交叉二聚体能够彻底发生光解,首先生成原来的反式单体,所生成的反式单体容易发生异构化而生成顺式单体,最终建立起反顺异构化平衡.  相似文献   

15.
Conclusions The conditions were found for the hydrosilylation of CH2=CHSi(OC2H5)3 with triorganylsilanes in the presence of H2PtCl6 · 6H2O in isopropanol, which assured a high yield (>90%) of the 1-(triorganylsilyl)-2-(tri-ethoxysilyl)ethanes. These conditions were used to synthesize 27 new 1-(triorganylsilyl)-2-(triethoxysilyl)-ethanes.The addition of (C2H5O)3SiH to (CH2=CHSi(CH3)3 in the presence of the same catalyst gave 1-(trimethyl-silyl)-2-(triethoxysilyl)ethane in 98.6% yield.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 7, pp. 1622–1625, July, 1976.  相似文献   

16.
Guido Verniest 《Tetrahedron》2005,61(19):4631-4637
The synthesis of chlorinated 2-(hydroxymethyl)-, 2-(alkoxymethyl)- and 2-(aminomethyl)pyrroles via aromatization of 2-aryl-3,3-dichloro-5-(bromomethyl)pyrrolines and via reduction of 2-formyl- and 2-cyanopyrroles is described. The former methodology also provided new 2-[(alkyl- or phenylamino)methyl]pyrroles and a 2-(phosphonomethyl)pyrrole. Halogenated and methylene-spaced functionalized pyrroles are of particular interest for their pronounced physiological activities.  相似文献   

17.
The preparation and resolution of two new axially chiral quinazoline-containing phosphinamine ligands, 2-(2-pyridyl)-Quinazolinap and 2-(2-pyrazinyl)-Quinazolinap, is described. The ligands were synthesised in good yield over eight steps and included two Pd-catalysed reactions, a Suzuki coupling to form the biaryl linkage and the introduction of the diphenylphosphino group, as the key transformations. The racemic ligands were resolved via the fractional crystallisation of diastereomeric palladacycles derived from (+)-di-μ-chlorobis{(R)-dimethyl[1-(1-naphthyl)ethyl]aminato-C2,N}dipalladium (II) X-ray crystal structures of the (S,R)-2-pyridyl- and (S,R)-2-pyrazinyl-palladacycles are included. Displacement of the resolving agent by reaction with 1,2-bis(diphenylphosphino)ethane gave enantiopure 2-(2-pyridyl)-Quinazolinap and 2-(2-pyrazinyl)-Quinazolinap, new atropisomeric phosphinamine ligands for asymmetric catalysis. These ligands were applied in the palladium-catalysed allylic substitution of 1,3-diphenylprop-2-enyl acetate resulting in moderate conversions and enantioselectivities of up to 81%.  相似文献   

18.
The synthesis of novel 2-(2-furyl)-cis-3-hydroxychro-manones(3a-c) has been achieved from 3-(2-furyl)-1-(2-hydroxy-aryl)-2-enones (1a-c) via acid catalyzed hydrolysis of dimethylacetals (2a-c), formed by hypervalent iodine oxidation using iodobenzene diacetate in methanolic potassium hydroxide. Action of dil. alkali on 3a and 3b provides a new synthesis of 2-(2-furyl)-3-hydroxychromones (6a, 6b).  相似文献   

19.
Reaction of 1,3-dicyanotetrafluorobenzene with 2 equiv of (trimethylsilyl)iminophosphoranes gave the disubstituted derivatives 4,6-(CN)(2)C(6)F(2)-1,3-AB: 1, A = B = (N=PPh(3)); 2, A = B = (N=PPh(2)Me); and 3, A = (N=PPh(3)), B = (N=PPh(2)Me). Monosubstituted compounds of the type 2,4-(CN)(2)C(6)F(3)-1-A; notably 4, A = (N=PPh(3)), and 5, A = (N=PPh(2)Me), were readily obtained by reaction of 1 molar equiv of the silylated iminophosphorane with the cyanofluoro aromatic. Substitution of the fluorine para to the CN group(s) occurs in all cases. Reactions of 1,2- and 1,4-dicyanotetrafluorobenzene with (trimethylsilyl)iminophosphoranes gave only monosubstituted derivatives 3,4-(CN)(2)C(6)F(3)-1-A (6, A = (N=PPh(3)), and 7, A = (N=PPh(2)Me)) and 2,5-(CN)(2)C(6)F(3)-1-A (8, A = (N=PPh(3)), and 9, A = (N=PPh(2)Me)), respectively, as the result of electronic deactivation of the second substitutional point. 1, 4,6-(CN)(2)C(6)F(2)-1,3-(N=PPh(3)), 2, 4,6-(CN)(2)C(6)F(2)-1,3-(N=PPh(2)Me)(2), and 3, 4,6-(CN)(2)C(6)F(2)-1-(N=PPh(3))-3-(N=PPh(2)Me) have been structurally characterized. For 1 (at 21 degrees C), monoclinic, C2/(c) (No. 15), a = 15.289(2) ?, b = 10.196(1) ?, c = 23.491(6) ?, beta = 91.63(2) degrees, V = 3660(2) ?(3), and Z = 4. The P=N bond length is 1.579(2) ? and the P(V)-N-C(phenyl) angle is 134.0(2) degrees. For 2, (at 21 degrees C) monoclinic, C2/(c) (No. 15), a = 18.694(2) ?, b = 8.576(1) ?, c = 40.084(4) ?, beta = 94.00(1) degrees, V = 6411(2) ?(3), and Z = 8. The P(1)=N(1) bond length is 1.570(4) ?, the P(2)=N(2) bond length is 1.589(3) ?, the P(1)-N(1)-C(14) angle is 131.6(3) degrees, and the P(2)-N(2)-C(16) angle is 131.3(3) degrees. For 3, (at -80 degrees C) monoclinic, P2(1)/c (No. 14), a = 9.210(1) ?, b = 18.113(2) ?, c = 20.015(2) ?, beta = 100.07(1) degrees, V = 3287(2) ?(3), and Z = 4. The P(1)=N(1) bond length (PPh(3) group) is 1.567(4) ?, the P(2)=N(2) bond length (PPh(2)Me group) is 1.581(5) ?, the P(1)-N(1)-C(1) angle is 140.4(4) degrees, and the P(2)-N(2)-C(3) angle is 129.4(4) degrees. These new multifunctional chelating ligands readily react with [Rh(cod)Cl](2) and AgClO(4) to give cationic Rh(I) complexes in which the imine and/or the nitrile groups are coordinated to the Rh center.  相似文献   

20.
Some new syntheses of 1-[2′-(ethylsulfonyl)ethyl]-2-methyl-5-nitroimidazole (IV), a new antitrichomonal agent are described. The most successful method proved to be alkylation of sodium ethanesulfinate (XXI) with 1-(2′-haloethyl)-2-methyl-5-nitroimidazoles (1a,b) in dimethylformamide.  相似文献   

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