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1.
为实现多种活性成分的有效叠加和为药物筛选提供先导化合物, 以1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酸为初始原料, 依次合成1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酰氯、1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酰基异硫氰酸酯, 再与取代苯并噻唑肼反应生成了8个未见报道的N-取代苯并噻唑-2-氨基-N'-取代吡唑-4-甲酰基硫脲. 采用超声波催化法合成了标题化合物, 并与加热回流的常规方法进行了对比. 超声波催化法具有操作简单、反应时间短、条件温和、产率高、副反应少等优点, 为此类化合物的合成提供了一种有效的新方法. 标题化合物经元素分析, IR, 1H NMR确证结构. 相似文献
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O,O'-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性 总被引:1,自引:0,他引:1
采用无溶剂无催化剂合成方法, 分别进行了以O,O'-二烷基亚磷酸酯、3,4,5-三甲氧基苯甲醛、2-氨基取代苯并噻唑为原料的类Mannich一锅法合成反应研究, 经合成筛选, 优选出控制反应温度100 ℃, 无溶剂、无催化剂加热反应120 min的合成方法, 实验结果表明该方法经济、简便、对环境友好. 经元素分析, IR, 1H NMR, 13C NMR对所合成的化合物进行了结构确认和表征. 培养并测定了化合物4a的晶体结构. 初步生物活性测试表明, 化合物具有一定的抗烟草花叶病毒活性. 相似文献
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新型3-萘基-1,3-噻唑烷-4-酮衍生物的微波促进合成及其抗菌活性研究 总被引:3,自引:1,他引:2
利用微波促进的多组分一锅法, 在封管条件下, 以萘胺、芳醛和巯基乙酸为原料, 4-二甲氨基吡啶(DMAP)/N,N’-二环已基碳二亚胺(DCC)为催化剂, 合成了系列新的噻唑烷酮衍生物, 该反应具有时间短、操作简便等优点. 目标化合物通过IR, NMR, MS和元素分析等方法确定结构. 初步测试了化合物对丁香假单胞杆菌黄瓜角斑病菌致病变种、番茄灰霉病菌和黄瓜白粉病菌抑制活性, 结果表明: 部分化合物对黄瓜白粉病菌有显著抑制作用, 但对前两种植物病菌抑制效果不明显. 相似文献
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红霉素9,11-亚胺醚和乙腈分子加合物的合成和晶体结构 总被引:1,自引:0,他引:1
通过控制红霉素A (E)肟的贝克曼重排反应条件合成了一种关键中间体红霉素9,11-亚胺醚, 该化合物可与乙腈形成稳定的分子加合物(摩尔比为1∶1), 未见文献报道. 阐述了该化合物的合成、晶体结构、晶体学数据和结构参数. 该化合物为无色透明晶体, 属单斜晶系, 空间群P21. 对该加合物和已知化合物红霉素6,9-亚胺醚晶体结构的对照解析, 有助于对重排反应机理、异构化机理和两异构体还原差异性的分析, 对重排反应和还原反应起到积极的指导作用. 相似文献
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3-烯-1,5-二炔是许多烯二炔类抗癌抗生素和发光材料的重要片断. 发展了一种高选择性合成E-烯二炔化合物的两步法: (1) CuBr2为卤化剂, 温和高效合成双卤代烯烃; (2)通过双卤代烯烃和末端炔烃的Sonogashira偶联反应构建烯二炔化合物. 相似文献
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2-芳基硫代芳胺的结构广泛存在于许多具有重要生理、药理活性的天然产物、药物以及材料当中, 研究此类结构的构建对这些化合物的合成路线设计可以提供新的思路. 传统合成2-芳基硫代芳胺, 常需多步骤或高温、强碱条件下进行, 能进行此类反应的反应物有限, 所得产物收率不高. 选用三氟乙酰基作为芳胺氮原子上的保护基, 利用三氟乙酰基的邻位促进效应, 并采用碘化亚铜/L-脯氨酸的催化体系, 在乙二醇二甲醚中, 碳酸钾为碱, 于60 ℃一步实现N-三氟乙酰基邻碘代苯胺与芳基硫酚的偶联, 以高产率获得了N-三氟乙酰基-2-芳基硫代芳胺. 反应条件温和, 催化体系价廉易得, 反应操作简便. 相似文献
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新型含吡唑基的查尔酮的合成、表征及晶体结构 总被引:2,自引:0,他引:2
以2种1-苯基-3-甲基-5-对甲苯氧基-吡唑-4-甲醛为原料, 在强碱条件下与苯乙酮(取代苯乙酮)发生羟醛缩合, 高产率地合成出10种新型含吡唑基的查尔酮. 化合物的结构经元素分析, IR和1H NMR确认. 并用X射线衍射法测定了化合物4c的晶体结构. 化合物4c属三斜晶系, 空间群P-1, 晶胞参数: a=1.0225(2) nm, b=1.4263(3) nm, c=1.6718(3) nm, α=110.32(3)°, β=106.30(3)°, γ=98.11(3)°, Mr=428.90, V=2.1159(7) nm3, Dc=1.346 Mg/m3, Z=2, F(000)=896. 相似文献
11.
1,2-Dihydro-3H-imidazo[1,5-a]benzimidazoles (6), 1-oxo-1,2-dihydro-3H-imidazo[ 1,5-a] benzimidazoles (8), 3H-imidazo[1,5-a]benzimidazoles (7), 3-oxo-1,2,3,4-tetrahydro-pyrazino[1,2-a] benzimidazoles (12), and 3,4-dioxo-1,2,3,4-tetrahydro-pyrazino[1,2-a]benzinudazoles (13) were synthesized from 2-α-aminobenzyl (benzhydryl)-benzimidazoles (2). 相似文献
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V. P. Kruglenko V. P. Gnidets N. A. Klyuev M. V. Povstyanoi 《Chemistry of Heterocyclic Compounds》1989,25(8):928-931
2-[(-Ethyl-, arylimino)phenethyl]-1,2,4-triazino[2,3-a]benzimidazoles were obtained by reaction of 2-aroylmethyl-1,2,4-triazino[2,3-a]benzimidazol-4H-3-ones with ethyl(aryl)amines or urea. By the action of phosphorus oxychloride, these benzimidazoles cyclize into substituted pyrrolo[2,3-e]-1,2,4-triazino[2,3-a]benzimidazoles, heating of which in polyphosphoric acid leads to the formation of furo[2,3-e]-1,2,4-triazino[2,3-a]benzimidazoles, while by the action of P4S10, they are transformed into thieno[2,3-e]-1,2,4-triazino[2,3-a]benzimidazoles.For Communication 20, see [1].Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1109–1113, August, 1989. 相似文献
13.
Gheorghe Roman 《Central European Journal of Chemistry》2012,10(5):1516-1526
Benzimidazole, benzimidazoles diversely substituted at position 2, and 5,6-dimethylbenzimidazole have been alkylated at N
1 with ketonic Mannich bases derived from acetophenones, acetylnaphthalenes, 2-acetylthiophene and 1-tetralone to afford a
series of novel 1-(3-oxopropyl)benzimidazoles. The reduction of these transamination products with NaBH4 in methanol produced the corresponding 1-(3-hydroxypropyl)benzimidazoles in excellent yields.
相似文献
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Zongjie Gan Qingqiang Tian Suqin Shang Wen Luo Zeshu Dai Huajun Wang Dan Li Xuetong Wang Jianyong Yuan 《Tetrahedron》2018,74(52):7450-7456
A facile, general, and economical synthesis of diversely functionalized benzimidazoles and 2-substituted benzimidazoles has been realized via the imidazolium chloride-catalyzed cyclization of o-phenylenediamines with DMF derivatives. This protocol shows a broad substrate scope for aliphatic, aromatic, and heteroaromatic amides. A series of benzimidazoles and 2-substituted benzimidazoles have been obtained in moderate to excellent yields. 相似文献
15.
By reaction of the appropriate 2-(ω-chloroalkyl)benzimidazoles with thiourea, 2-(α-mercaptoalkyl)benzimidazoles (IV) have been prepared. The attempted preparation of 2-(β- and γ-mercaptoalkyl)benzimidazoles failed. β-Elimination was observed by alkaline treatment of S-[2-(2-benzimidazolyl)-propyl]isothiuronium chloride (VII), whereas 2-(γ-chlorobutyl)benzimidazoles did not give an isothiuronium chloride. 相似文献
16.
A microwave-assisted general method for the synthesis of 2-aminovinyl benzimidazoles has been developed.Treatment of the 1,2-phenylenediamines and N-arylated/N,N-dialkylated 3-aminoacroleins with bis(cyclopentadienyl)zirconium(IV) dichloride(Cp2Zr Cl2) as the catalyst under microwave irradiation for 3–5 min followed by in situ Mn O2 oxidation afforded thirteen 2-aminovinyl benzimidazoles in good yields. 相似文献
17.
Vaibhav N. Khose Marina E. John Anita D. Pandey Anil V. Karnik 《Tetrahedron: Asymmetry》2017,28(10):1233-1289
Chiral aspects of benzimidazoles have been over-shadowed for a long time due to the large number of reports on benzimidazoles in the medical field in numerous categories of therapeutic agents. The vigorous research activity in chiral applications of benzimidazole derivatives started after bifunctional benzimidazoles made their appearance especially in the last 2–3 decades. Thus, chiral benzimidazoles form a comparatively young branch of chiral chemistry. The presence of pyridine and pyrrole type of nitrogens along with the fused benzene ring confer on this class of molecules, special properties including useful nucleophilicity, hydrogen bonding ability and a rigid backbone, all of which play decisive roles in proven chiral applications. The present review aims to cover the synthetic routes to access chiral benzimidazoles and their applications in a plethora of chiral fields including enantioselective organocatalysis, metal-based catalysis, asymmetric transformations involving benzimidazole-N-heterocyclic carbenes, kinetic resolution, benzimidazole-based macrocyclic hosts in chiral supramolecular chemistry and other miscellaneous chiral applications. 相似文献
18.
Keitaro Senga Roland K. Robins Darrell E. O'Brien 《Journal of heterocyclic chemistry》1975,12(5):899-901
The synthesis of a new class of tetracyclic bridgehead heterocycle pyrazolo[1′,5′:1,2]-1,3,5-triazino[5,6-a] benzimidazoles is reported. The key intermediate 2-(3-aminopyrazol-2-yl)benzimidazoles were prepared by the reaction of 2-hydrazinobenzimidazole with an appropriate reagent such as ethyl ethoxymethylenecyanoacetate, ethoxymethylenemalononitrile, β-cyanoacetophenone or α-formylphenylacetonitrile. The treatment of these key intermediates with triethylorthoesters afforded the corresponding pyrazolo[1′,5′:1,2]-1,3,5-triazino[5,6-a]benzimidazoles. 相似文献
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The 2-nitrophenylhydrazones 2 of D-arabino-2-hexulopyranosonic acid, D-arabinose, D-galactose and D-galacturonic acid are used as precursors to form chiral functionalized 1,2,4-benzotriazines and benzimidazoles by reductive cyclization methods. Catalytic hydrogenation provided the amine derivatives which are cyclized and air oxidized in alkaline solution to yield the novel 1,2,4-benzotriazines 3 as the main products, while on acid catalysis the benzimidazoles 4 are formed. 相似文献