共查询到20条相似文献,搜索用时 125 毫秒
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以2-吲哚酮为先导化合物,设计合成一系列2-吗啉基-1-丙基-1H-吲哚-3-取代酰腙类化合物.目标化合物结构经核磁共振波谱(1H NMR和13C NMR)和高分辨质谱仪(HRMS)进行确证.采用浊度法测试了目标化合物的离体抑菌活性,抑菌活性测试结果表明:目标化合物对柑橘溃疡病菌(Xanthomonas axonopodis pv.Citri,X.citri)、烟草青枯病菌(Ralstonia.Solanacearum,R.solanacearum)和水稻白叶枯病菌(Xanthomonas oryzae pv.Oryzae,X.oryzae)均表现出一定的抑制活性.化合物2-氰基-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)乙酰肼(12a)、4-氯-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)苯甲酰肼(12c)、4-氟-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)苯甲酰肼(12f)、N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)-4-硝基苯甲酰肼(12k)和N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)异烟肼(12m)表现出较好的抑制活性;化合物12a、12c、12f、12k和12m对水稻白叶枯病菌的EC50为73.79、61.94、59.70、36.72和82.79μg/m L,抑制活性优于对照药叶枯唑和噻菌铜(EC50分别为92.4、120.22μg/m L). 相似文献
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以仲胺、氧杂环丁-3-酮和三甲基氰硅烷为原料,无水甲醇为溶剂,无需催化剂,一步反应合成目标化合物3-仲氨基氧杂环丁烷-3-腈衍生物(1a~1d),产物结构经1H NMR和ESI-MS表征。并以异吲哚啉、氧杂环丁-3-酮和三甲基氰硅烷的反应为模型反应,考察影响产物1a收率的主要因素,确定最佳反应条件为:物料摩尔比为n(异吲哚啉): n(氧杂环丁-3-酮): n(三甲基氰硅烷)= 2.0 : 1 : 2.5;反应溶剂为无水甲醇,在65 ℃反应6 h。在最佳反应条件下,化合物1a收率78.3 %。对于目标化合物的应用进行了研究,发现化合物1a与苯基溴化镁在四氢呋喃溶剂中,室温反应5 h,得到2-(3-苯基氧杂环丁烷-3-基)异吲哚啉(4)和 [3-(异吲哚啉-2-基) 氧杂环丁烷-3-基](苯基)甲酮(5),收率分别为40.1 %和31.5 %。 相似文献
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以苯胺为原料,通过传统方法合成靛红。靛红与盐酸羟胺反应生成3-羟基亚氨基-2-吲哚酮,再通过钯碳加氢还原生成3-氨基-2-吲哚酮。合成中,采用钯碳加氢的还原方式,产物收率提高(收率82.76%,较文献提高了11.8%),后处理更简单,而且该方法可操作性高,成本低,产生三废少,是一条适合大规模生产3-氨基-2-吲哚酮的新合成工艺路线。 相似文献
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本文研究了十七种2-芳基吲哚(1a-1q)在甲醇-乙酸介质中的亚甲基蓝(MB)敏化光氧化反应, 发现有十五种吲哚(1a-1o)以85%-95%的产率给出2,2'-二芳基-[2,3'-联-1H-吲哚]-3(2H)-酮(2a-2o), 而2-(4-硝基苯基]吲哚(1p)和2-联苯基吲哚(1q)则分别生成2-甲氧基-2-(4-硝基苯基)-1,2-二氢-3H-吲哚-3-酮(7p)和2-联苯基-4H-3,1-苯并恶嗪-4-酮(11q), 其中7p在分离过程中失去甲醇分子给出2-(4-硝基苯基)-3H-吲哚-3-酮(10p)。 相似文献
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Aly H. Atta 《中国化学会会志》2006,53(3):663-667
Some spiro indolone derivatives 5a,b and 6 were synthesized through one‐pot synthesis via the ternary condensation of 1H‐indole‐2,3‐dione 1 , 3‐methyl‐1‐phenyl‐2‐pyrazolin‐5‐one 2 and active methylenes, namely malononitrile, ethyl cyanoacetate 4a,b and pyrazolone 2 , respectively. The same derivatives can be obtained via other methods, through reactions of 3‐[3‐methyl‐5‐oxo‐1‐phenyl‐1,5‐dihydro‐pyrazol‐(4Z)‐ylidene]‐1,3‐dihydro‐indol‐2‐one 3 with the corresponding active methylenes. Reaction of 3 with amines and with ethyl vinyl ether was studied. 相似文献
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Vladimír Mrkvička Antonín Lyčka Robert Vícha Antonín Klásek 《Helvetica chimica acta》2011,94(1):78-91
3‐Hydroxyquinoline‐2,4‐diones 1 react with isocyanates to give novel 1,2,3,4‐tetrahydro‐2,4‐dioxoquinolin‐3‐yl (alkyl/aryl)carbamates 2 and/or 1,9b‐dihydro‐9b‐hydroxyoxazolo[5,4‐c]quinoline‐2,4(3aH,5H)‐diones 3 . Both of these compounds are converted, by boiling in cyclohexylbenzene solution in the presence of Ph3P or 4‐(dimethylamino)pyridine, to give 3‐(acyloxy)‐1,3‐dihydro‐2H‐indol‐2‐ones 8 . All compounds were characterized by IR, and 1H‐ and 13C‐NMR spectroscopy, as well as by EI mass spectrometry. 相似文献
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1-甲基-2-苯基吲哚(1)在甲醇中的琥红(RB)敏化单重态氧反应生成1-甲基-2-甲基氧-2-苯基-1, 2-二氢-3H-吲哚-3-酮(4)和1-甲基-2-羟基-2-苯基-1, 2-二氢-3H-吲哚-3-酮(6), 后者在强碱性介质下发生苯乙醇酸型重排生成1-甲基-3-羟基-3-苯基氧化吲哚(14)。研究了6的溶剂分解反应以及外加碱对光氧化反应的影响。探讨了光氧化产物的形成途径。结果表明: 4系两性离子中间体2的溶剂捕获、脱水产物, 而6则系二氧杂环丁烷中间体7的裂解、抽氢产物。 相似文献
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The proline‐catalyzed addition of various aliphatic aldehydes to sterically hindered 2‐aryl‐substituted 3H‐indol‐3‐ones affords 2,2‐disubstituted 2,3‐dihydro‐1H‐indol‐3‐one derivatives with excellent enantioselectivities. In addition, the synthesis of a chiral derivative, (S)‐2‐(2‐bromophenyl)‐2,3‐dihydro‐2‐(2‐hydroxyethyl)‐1H‐indol‐3‐one, which can be used as an intermediate for the preparation of the natural product hinckdentine A was accomplished with a high level of enantioselectivity. 相似文献
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A palladium‐catalyzed intramolecular α‐arylation of an amide in the presence of a bulky chiral N‐heterocyclic carbene ligand is the key step in the first catalytic synthesis of (3R)‐6‐chloro‐3‐(3‐chlorobenzyl)‐1,3‐dihydro‐3‐(3‐methoxyphenyl)‐2H‐indol‐2‐one ((R)‐ 5 ). This oxindole, in racemic form, had been shown previously to be an anticancer agent. (R)‐ 5 was obtained with an overall yield of 45% and with 96% enantioselectivity. 相似文献
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The Synthesis of New Heterocycles Using 2‐(4‐Chloro‐1,3‐dihydro‐3,3,7‐trimethyl‐2H‐indol‐2‐ylidene) Propanedial
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Maryam Alyari Mehdi M. Baradarani Arash Afghan John A. Joule 《Journal of heterocyclic chemistry》2014,51(3):854-859
4‐Chloro‐2,3,3,7‐tetramethyl‐3H‐indole (an indolenine) was produced by the reaction of 5‐chloro‐2‐methylphenylhydrazine hydrochloride with 3‐methylbutan‐2‐one via Fischer reaction. Exposure of the indolenine to the Vilsmeier reagent at 50°C produced a β‐diformyl compound, 2‐(4‐chloro‐1,3‐dihydro‐3,3,7‐trimethyl‐2H‐indol‐2‐ylidene)propanedial. This dialdehyde was reacted with arylhydrazines, acetamidinium chloride, urea, thiourea, guanidinium chloride, and cyanoacetamide to give various 5‐membered and 6‐membered heterocyclic products, each carrying a 4‐chloro‐3,3,7‐trimethyl‐3H‐indol‐2‐yl unit as a substituent, in excellent yields. 相似文献
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Lactone analogues of 3‐substituted oxindoles (=1,3‐dihydro‐2H‐indol‐2‐ones) and nonbenzoid oxa‐analogous isoindigoid or nonbenzoid isoindigoid dyes were prepared by the reactions of furan‐2,3‐diones with oxindole and Lawesson reagent (Schemes 1 and 3), respectively. So, new derivatives of 2‐oxobutanoic acid, bis‐furanone, and bis‐pyrrolone, which are potentially biologically active compounds, were synthesized for the first time. 相似文献
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Diastereoselective Synthesis of (Z)‐6‐(2‐Oxo‐1,2‐dihydro‐3H‐indol‐3‐ylidene)‐3,3a,9,9a‐tetrahydroimidazo[4,5‐e]thiazolo[3,2‐b]‐1,2,4‐triazin‐2,7(1H,6H)‐diones
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Galina A. Gazieva Ekaterina A. Shishkova Ludmila B. Kulikova Natal'ya G. Kolotyrkina Natal'ya V. Sigay Angelina N. Kravchenko 《Journal of heterocyclic chemistry》2014,51(4):921-926
Two efficient and diastereoselective procedures for the synthesis of (Z)‐6‐(2‐oxo‐1,2‐dihydro‐3H‐indol‐3‐ylidene)‐3,3a,9,9a‐tetrahydroimidazo[4,5‐e]thiazolo[3,2‐b]‐1,2,4‐triazin‐2,7(1H,6H)‐diones by aldol‐crotonic condensation of 1,3‐dimethyl‐3a,9a‐diphenyl‐3,3a,9,9a‐tetrahydroimidazo[4,5‐e]thiazolo[3,2‐b]‐1,2,4‐triazin‐2,7(1H,6H)‐dione with isatins under acidic or basic catalysis are reported. Isomerization in (Z)‐7‐(1‐allyl‐2‐oxo‐1,2‐dihydro‐3H‐indol‐3‐ylidene)‐1,3‐dimethyl‐3a,9a‐diphenyl‐1,3a,4,9a‐tetrahydroimidazo[4,5‐e]thiazolo[2,3‐c]‐1,2,4‐triazin‐2,8(3H,7H)‐dione was observed under basic conditions. 相似文献
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[2,3’-联-1H-吲哚]-3(2H)-酮衍生物(1a~1c)在甲醇中的单重态氧反应给出溶剂捕捉产物4,后者在分离过程中脱去甲醇分子生成5。考察了标题化合物分子中二氢吲哚酮结构单元以及吲哚结构单元在单重态氧反应中的作用。并探讨了反应机理。 相似文献