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1,2-二芳基乙二酮与1,2-苯二胺在室温醋酸溶液中反应数分钟,生成2,3-二芳基一喹喔啉.反应时间短(1~10min),产率高(90%~97%),反应条件温和,操作简便. 相似文献
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以邻苯二胺、丙二酸和果糖为主要原料,经Knoevenagel反应合成了一个新的芳稠杂环化合物——1,1-二(苯并咪唑-2-基)-2-(喹喔啉-2-基)乙烯(4),收率78.61%,其结构经1H NMR,IR和元素分析表征。利用UVVis和FL研究了4的光学性能,结果表明:4的最大吸收峰位于259 nm和383 nm;在320 nm激发波长激发下,4的λem位于495 nm,具有显著的日光紫外线吸收性能;TG/DTA分析表明:4的熔点为320℃,初始分解温度为402℃,具有良好的热稳定性。 相似文献
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喹喔啉和1,2,3-三唑都是具有广泛生物活性的杂环结构母体。本文基于药物设计的拼合原理,以简单易得的邻苯二胺、苯乙炔及有机叠氮为原料,通过三组分"两步一锅法"将喹喔啉和1,2,3-三唑活性亚结构进行拼接,合成了一系列共14个新型喹喔啉-三唑衍生物(3a~3n)。该法操作简单,无需分离中间体,两步总产率52.6%~78.4%。合成的目标化合物结构经~1H NMR、~(13)C NMR和HRMS确证。初步体外抗肿瘤活性测试表明,合成的目标化合物具有一定的抗肿瘤活性。 相似文献
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十一种2,3-二取代喹喔啉-1,4-二氧化物抗菌剂的合成与谱学研究 总被引:3,自引:0,他引:3
采用直接氧化法和Beirut反应合成了十一种抗菌剂2,3-二取代喹喔啉-1。4-二氧化物.给出了完整的UV,IR,NMR数据和有关谱学特性.EPR研究表明这些N-氧化物在溶液光解过程中生成稳定的顺磁物.从含有2,3-环丁亚基喹喔啉-1,4-氧化物(2g)的氯仿溶液光解体系记录的EPR谱得到9.69G(1N)、3.59G(2H),1.25G(2H)和0.76G(1H)等超精细分裂值,指认为1-羟基-2,3-环丁亚甲基喹喔啉-4-氧基(4).指出喹喔啉-1,4-氧化物与对萘醌化合物有结构、物性的类似性. 相似文献
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取代喹喔啉-1,4-二氧化物合成方法的改进 总被引:1,自引:0,他引:1
苯并呋咱-1-氧化物(1)分别与1,3-二酮、β-酮酯(2a~c)在氢氧化钾(钠)的醇溶液中反应,合成了取代喹喔啉-1,4-二氧化物(3a~c),产率较高。将本方法与在有机胺中合成这些化合物的Beirut反应作了比较,并且讨论了溶剂和反应温度对产物的影响。 相似文献
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设计了一个有机合成综合性实验,该实验以邻苯二胺、乙酰乙酸乙酯、苯甲醛为原料,在磷钨酸催化、乙醇作溶剂、冰水浴条件下一步3组分合成1,5-苯并二氮杂卓化合物。实验实现了该化合物由原来的多步合成转化为一步合成,不但避免了中间产物的分离,而且反应条件温和、操作简便、产物收率高、环境友好等,是绿色化学在有机合成中的实际应用,以及现代有机合成方法的具体体现,也是培养学生创新实验能力的较好途径和方法。 相似文献
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三氯化稀土有效地催化了邻苯二胺与一系列α,β-不饱和酮的反应,在温和条件下以中等到高的收率生成1,5-苯并二氮杂卓。 相似文献
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Synthesis and Antimicrobial Activities of Novel 2‐[substituted‐1H‐pyrazol‐4‐yl] Benzothiazoles,Benzoxazoles, and Benzimidazoles 下载免费PDF全文
Vikas S. Padalkar Bhushan N. Borse Vinod D. Gupta Kiran R. Phatangare Vikas S. Patil Nagaian Sekar 《Journal of heterocyclic chemistry》2016,53(5):1347-1355
In an endeavor to find a new class of antimicrobial agents, a series of novel substituted benzimidazole, benzoxazole, and benzothiazole derivatives 6 containing pyrazole moiety have been synthesized by reaction of 3‐aryl‐4‐formyl pyrazole 4 with substituted phenylenediamine or o‐aminophenol or o‐aminothiophenol 5 . Reaction of phenyl hydrazine or 2‐hydrazinopyridine 1 with substituted acetophenones 2 gave the corresponding hydrazones 3 , which on Vilsmeier–Haack reaction with POCl3–DMF gave substituted 3‐aryl‐4‐formyl pyrazoles 4 . All final compounds 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j , 6k were evaluated for in vitro antibacterial activities against Escherichia coli and Staphylococcus aureus strains and in vitro antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. The antimicrobial activities were expressed as the minimum inhibitory concentration in µg/mL. The compound containing benzimidazole and benzoxazole moiety gave better antibacterial and antifungal activities than benzothiazole compounds. 相似文献
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A novel conversion of 2, 4‐diaryl‐2, 3‐dihydro‐1 H‐1, 5‐benzodiazepins into 2, 4‐diaryl‐3 H‐1, 5‐benzodiazepines by the reaction with m‐chloroperbenzoic acid (MCPBA) was reported. 相似文献
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Raquel G. Jacob Ctia S. Radatz Mariele B. Rodrigues Diego Alves Gelson Perin Eder J. Lenardo Lucielli Savegnago 《Heteroatom Chemistry》2011,22(2):180-185
A general and easy method for the synthesis of several 1‐H‐1,5‐benzodiazepines using SiO2/ZnCl2 under solvent‐free conditions is described. This efficient and improved method furnishes selectively and in good yields the corresponding 1‐H‐1,5‐benzodiazepines derivatives starting from o‐phenylenediamine and cyclic or acyclic ketones. The catalytic system was reused up four times, and the use of focused microwaves accelerates the reaction. © 2011 Wiley Periodicals, Inc. Heteroatom Chem 22:180–185, 2011; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.20674 相似文献
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Richard A. Bunce Christopher L. Smith Jason R. Lewis 《Journal of heterocyclic chemistry》2004,41(6):963-970
A tandem reduction‐reductive amination reaction has been applied to the synthesis of (±)‐4‐alkyl‐2,3,4,5‐tetrahydro‐1,5‐benzoxazepines and (±)‐4‐alkyl‐1‐benzoyl‐2,3,4,5‐tetrahydro‐1H‐1,5‐benzodiazepines. The nitro aldehydes and ketones required for 1,5‐benzoxazepine ring closures were prepared by nucleophilic aromatic substitution of the alkoxides from several 3‐buten‐1‐ol derivatives with 2‐fluoro‐1‐nitrobenzene followed by ozonolysis. Precursors for the 1,5‐benzodiazepines were prepared by similar addition of N‐(3‐butenyl)benzamide anions to 2‐fluoro‐1‐nitrobenzene followed by ozonolysis. Catalytic hydrogenation of the nitro carbonyl compounds using 5% palladium‐on‐carbon in methanol then gave the target heterocycles by a tandem reduction‐reductive amination sequence. The 1,5‐benzoxazepines were isolated in high yield following chromatographic purification; the 1,5‐benzodiazepines were isolated as solids directly from the hydrogenation mixture and possessed differentiated functionality on the two nitrogen atoms. 相似文献
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2,4‐Disubstituted 1‐benzoyl‐2,3‐dihydro‐1H‐1,5‐benzodiazepines were oxidized by m‐chloroperbenzoic acid (MCPBA) to produce 1a,3‐disubstituted 4‐benzoyl‐1a,2,3,4‐tetrahydro‐oxazirino[2,3‐a][1,5]benzodiazepines, a novel tricyclic heterocyclic system. However, 2,4‐disubstituted 2,3‐dihydro‐1H‐1,5‐benzodiazepines were oxidized by MCPBA under the same conditions to give a 2,4‐disubstituted 2,3‐dihydro‐2‐hydroxy‐1H‐1,5‐benzodiazepine or a 2,4‐disubstituted 3H‐1,5‐benzodiazepine, respectively. We propose a hydroxylation mechanism of peracid oxidation. © 2000 John Wiley & Sons, Inc. Heteroatom Chem 11:158–162, 2000 相似文献
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Synthesis of N‐(1H‐imidazoline‐2‐yl)‐1H‐benzimidazol‐2‐amine was carried out under microwave irradiation (MWI) conditions. Dynamic 1H NMR investigation of N‐(1H‐imidazoline‐2‐yl)‐1H‐benzimidazol‐2‐amine compound was reported at temperature range of 223–333 K in DMF‐d7. Some physical parameters, such as coalescence temperature (Tc), the free energy of activation (ΔG??) and rate constant (k) values were calculated from its 1H NMR spectra at various temperatures. Electrochemical feature of this compound was investigated by cyclic (CV) and square wave voltammetry (SWV). 相似文献