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1.
微波辐射下2-[4-二-(4-氟苯)甲基]哌嗪乙酰腙化合物的合成 总被引:3,自引:0,他引:3
微波辐射条件下, 以丙酮作溶剂, 1-[二-(4-氟苯)甲基]哌嗪与氯乙酸乙酯反应得到2-[二-(4-氟苯)甲基]哌嗪乙酸乙酯(1), 1与水合肼在微波辐射条件下反应得到2-[二-(4-氟苯)甲基]哌嗪乙酰肼(2), 进一步在微波辐射条件下由2-[二- (4-氟苯)甲基]哌嗪乙酰肼(2)与取代芳香醛反应制得目标化合物3a~3f. 合成的6个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析、元素分析对其结构进行确证. 相似文献
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在微波作用、无催化剂的条件下合成3-芳基亚甲基-1,3-二氢-2H-吲哚-2-酮类化合物 总被引:3,自引:1,他引:3
用DMF作溶剂,无催化剂、微波辐射的条件下,使吲哚-2-酮(1)和醛、酮(2)发 生缩合反应,合成了3-芳基亚甲基-1,3-二氢-2H-吲哚-2-酮类化合物,时间短、 收率高。 相似文献
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发展了一种从3-(2-溴代苯甲酰基)-吲哚出发在无过渡金属参与下合成茚并吲哚酮类化合物的新方法。在甲苯/四氢呋喃(2∶1)混合溶剂中,3-(2-溴代苯甲酰基)-吲哚、正丁基锂和碘化锌原位生成的2-吲哚锌在碘化锂辅助下与芳基溴化物发生分子内加成-环化反应,合成了一系列取代的茚并-[1,2-b]吲哚-10(5H)-酮类化合物,且均获得了较好的收率。考察了溶剂、卤化锌、添加剂对产率的影响。 相似文献
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《化学研究与应用》2020,(5)
以对硝基苯肼为起始原料,采用费舍尔吲哚合成法合成中间体5-硝基吲哚-2-羧酸酯(3),经还原合成5-氨基吲哚-2-羧酸酯(4),再与氯甲酸苯酯合成酰胺(5),5在水合肼作用下形成2,5-碳酰肼吲哚(6),化合物6和取代醛反应,合成了7个2,5-二取代吲哚碳酰肼衍生物(7a~7g)。目标化合物经~1HNMR、~(13)CNMR、HR-MS结构确证。采用MTT法研究了目标化合物的细胞毒活性。结果显示,目标化合物对所选肿瘤细胞的增殖活性具有一定抑制作用。其中7c对宫颈癌细胞(Hela)、乳腺癌细胞(MCF-7)和人肝癌细胞(HepG-2)的抑制活性与阳性药顺铂活性相近。 相似文献
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为了研究HIV-1 Tat/PCAF BRD抑制剂的构效关系, 合成了6个3-芳氧基-1-丙胺类化合物. 以取代的2-硝基苯酚为起始原料, 在常规加热和微波辐射加热下与1,3-二溴丙烷反应合成3-(2-硝基芳氧基)-1-溴丙烷(3), 结果显示, 微波辐射加热比常规加热下的反应速度明显加快, 收率有所提高. 3和邻苯二甲酰亚胺钾进行N-烷基化反应合成了2-[3-(芳氧基)-丙基]二氢异吲哚-1,3-二酮, 再经肼解得到了目标化合物, 所有化合物的结构均经FTIR, 1H NMR, 13C NMR及HRMS确证. ELISA检测法测定了它们体外抑制HIV-1 Tat/PCAF BRD的活性, 并对影响活性的因素进行了讨论. 相似文献
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Wen Tao GAO* Zhuo ZHENG Department of Chemistry Jinzhou Teachers College Jinzhou Dalian Institute of Chemical Physics Chinese Academy of Science Dalian 《中国化学快报》2001,(2)
It is generally known that due to their special structures, tropolpone compounds demonstrate virtually the same aromaticity as benzene compounds, thus undergoing electrophilic substitution reactions with electrophilic reagents. The researches about this have been reported in many papers, especially about the reactions of 3-acetyltropolone1, 3-acetamidotropolone2, 3-cinnamoyltropolone3, 3-iso-propenyl-tropo-lone4, 3-(2-quinilinyl) tropolone5 with various electrophilic reagents. But, the substit… 相似文献
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Gutierrez-Lugo MT Woldemichael GM Singh MP Suarez PA Maiese WM Montenegro G Timmermann BN 《Natural product research》2005,19(7):645-652
Bioassay guided isolation of an antibacterial extract prepared from the fermentation broth of a Micromonospora sp. P1068 led to the isolation of eight compounds identified as (3R) 3,4',7-trihydroxy-isoflavanone (1), 3-hydroxydehydrodaidzein, daidzein (2), 3-methyl-1H-indole-2-carboxylic acid (3), 1H-indole-3-carboxaldehyde (4), 3-(p-hydroxyphenyl)-N-methylpropionamide, N-methylphloretamide (5), phenyl acetic acid (6), 2-hydroxy phenyl acetic acid (7) and 4-hydroxy-5-methoxy-benzoic acid (8). Compounds 1 and 5 were found to be novel chemical entities while 3 was isolated from a natural source for the first time. All compounds were evaluated for their antimicrobial activities against a panel of clinically significant microorganisms. Compound 4 was active against Staphylococcus aureus (MIC, 32 microg/ml), Enterococcus faecium (MIC, 32 microg/ml) and Escherichia coli (MIC, 64 microg/ml). 相似文献
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Shattat G Al-Qirim R Al-Hiari Y Sheikha GA Al-Qirim T El-Huneidi W Shahwan M 《Molecules (Basel, Switzerland)》2010,15(9):5840-5849
The lipid-lowering activity of a series of novel N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives has been studied in Triton WR-1339-induced hyperlipidemia in rats. The test animals were divided into four groups: control, hyperlipidemic, compound + 4% DMSO [C1: N-(2-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (1), C2: N-(3-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (2), C3: N-(4-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (3)]-treated and bezafibrate (BF)-treated. At a dose of 15 mg/Kg body weight, compounds 2, 3 and BF significantly reduced elevated plasma triglycerodes levels after 12 h. Moreover, high density lipoprotein-cholesterol levels were significantly increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for C1 which was inactive. In sum, it may be stated that the results of the present study demonstrated new properties of some N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives as potent lipid lowering agents and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role. 相似文献
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GUAN Ruqi CHAO Guoku YE Caiping WANG Yuxiang LIU Yanmei LI Haihua ZHAO Yajuan TAI Yulei 《高等学校化学研究》2014,30(2):284-288
Ru-B/γ-Al2O3 catalyst was prepared by reductant impregnation method,which was applied in the selective hydrogenation of ethyl 1H-indole-2-carboxylate for producing ethyl 2,3,3a,7a-tetrahydro-1H-indole-2-carboxylate with hydrogen as reductant.Furthermore,we discussed the influences of substrate concentration,reaction solvent,hydrogenation temperature,initial hydrogen pressure and reaction time on the catalytic performance of the as-prepared catalyst.The obtained Ru-B/γ-Al2O3 catalyst showed a high-efficiency for the selective hydrogenation of ethyl 1H-indole-2-carboxylate(>99% conversion and selectivity) in i-propanol used as solvent at a concentration of 10%(mass fraction) of ethyl 1H-indole-2-carboxylate,a pressure of hydrogen of 6 MPa and a reaction temperature of 373 K. 相似文献
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K. F. Suzdalev N. I. Vikrishchuk S. A. Tsiryulnik 《Russian Journal of General Chemistry》2020,90(4):572-578
One-pot synthesis of 3-vinyl substituted indoles containing 1,2-amino alcohol fragment at the nitrogen atom was performed by the reactions of 1-(oxiran-2-ylmethyl)-1H-indole-3-carbaldehyde with methylene-active compounds and amines. 相似文献
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Facile and green syntheses of substituted-2-(N-methylindole-3-carbonyl)-3-(N-methyl pyrrol-2-yl) acrylonitriles 6a–d are being reported. L-Proline has been utilized as an efficient and ecofriendly catalyst in aqueous medium for Knoevenagel condensation of pyrrole-2-carboxyaldehyde (1) and its N-methyl derivative (2) with the active methylene compounds 3-cyanoacetylindoles 3a–d at room temperature to afford substituted-2-(1H-indole-3-carbonyl)-3-(1H-pyrrol-2-yl)acrylonitriles 4a–d and substituted-2-(1H-indole-3-carbonyl)-3-(N-methylpyrrol-2-yl) acrylonitriles 5a–d respectively. Subsequently these products were treated with dimethyl sulfate (DMS) in polythylene glycol (PEG)–600 as an efficient and green solvent to afford the corresponding substituted-2-(N-methylindole-3-carbonyl)-3-(N-methylpyrrol-2-yl)acrylonitriles 6a–d. The antibacterial and antifungal activities of 4a–d, 5a–d, and 6a–d have been studied. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource: Full experimental and spectral details.] 相似文献
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ZHAO Chun-shen ZHAO Yan-fang CHAI Hui-fang GONG PingLiaoning Province Key Laboratory of Innovative Medicine Research Design Shenyang Pharmaceutical University Shenyang P. R. China 《高等学校化学研究》2006,22(5):577-583
IntroductionHepatitis B caused by a virus(HBV)is a commoninfectious disease in the world.According to WHO,700million people have been infected with HBVin theworld[1,2].HBV infection causes severe liver diseasesuch as cirrhosis and may also eventually lead… 相似文献
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Vikrishchuk N. I. Suzdalev K. F. Dranikova A. Yu. Tkachev V. V. Shilov G. V. 《Russian Journal of General Chemistry》2019,89(12):2369-2373
Russian Journal of General Chemistry - The reaction of 1-alkyl-2-chloro-1H-indole-3-carbaldehydes with 4-amino-5-alkyl(aryl)-4H-1,2,4-triazole-3-thiols afforded new heterocyclic compounds, namely... 相似文献
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Anshu Dandia Ruby Singh Kapil Arya 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3):551-564
A series of new spiro[3H-indole-3,2′-thiazolidine]-2,4′(1H)-diones (IV) and spiro[3H-indole-3,2′-tetrahydro-1,3-thiazine]-2,4′(1H)-diones (V) have been synthesized in 85–93% yield by the one-pot environmentally benign microwave induced technique involving the cyclocondensation of 3-arylimino-2H-indol-2-ones (III) with thioacids viz. mercapto aceticacid (a)/3-mercapto propionicacid (b) using montmorillonite KSF as inorganic solid support. Intermediates (III) were synthesized in situ by the reaction of indole-2,3-diones (I) and substituted anilines (II). The spiro compounds have been further subjected to solvent-free acetylation, aminoalkylation and thiation under microwave irradiation using solid supports. The synthesized compounds have been screened in vitro for antifungal activity against Rhizoctonia solani, Fusarium oxysporum, and Collectotrichum capsici, and antitubercular acivity against Mycobacterium tuberculosis. 相似文献
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吲哚啉螺萘并吡喃的合成和时间分辩光谱研究 总被引:3,自引:2,他引:1
螺萘并吡喃类化合物是一类重要的有机光致变色化合物,因可用作光敏、光信息和光记录材料,而引起人们的研究兴趣.其中对螺苯并吡喃和螺嗪两类化合物的开环机理有较多的文献报道[1,2],而对螺萘并吡喃的研究则少得多.我们合成了3个螺萘并吡喃化合物(其中SP1... 相似文献