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《有机化学》2017,(6)
从色醇出发,通过Sharpless环氧化、酰胺化、偶联和成盐四步反应合成了一系列新型的吲哚并四氢呋喃-咪唑盐杂合物,其结构经~1H NMR,~(13)CNMR,HRMS以及X射线单晶衍射确定.对合成的新化合物进行了体外抗肿瘤细胞毒活性筛选,结果表明,1-((3aR,8aS)-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8(8aH)-基)乙酮-3-(2-(萘-2-基)-2-氧乙基)-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐(20)和1-((3aR,8aS)-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8(8aH)-基)乙酮-3-(2-萘甲基))-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐(22)具有较好的体外肿瘤生长抑制活性,对SMMC-7721、MCF-7和SW-480肿瘤细胞株的活性均优于顺铂(DDP),1-((3aR,8aS)-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8(8a H)-基)乙酮-3-(2-溴苄基))-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐(24)对SW-480肿瘤细胞株表现出较好的选择性细胞毒活性,其IC_(50)值约为顺铂的2.0倍. 相似文献
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<正>近年来,聚合物太阳能电池(PSCs)以其重量轻、价格低廉、可通过印刷方式制备大面积柔性器件等潜在优势,得到了学术界和工业界的广泛关注,也是世界各国在新能源部署上的重要研究方向之一.窄带非富勒烯受体(如2,2’-[[6,6,12,12-四(4-己基苯基)-6,12-二氢二硫代[2,3-d:2’,3’-d’]-s-吲哚诺[1,2-b:5,6-b’]二噻吩-2,8-二基]双[亚甲基(3-氧代-1H-茚-2,1(3H)-二亚甲基)]]双[丙胺](ITIC)、2,2’-((2Z,2’Z)-((4,4,9,9-四(对己基苯)-4,9-二氢-S-引达省并二噻吩-2,7-二基)双(甲基亚基))-双-(3-氧代-2,3-二氢-1H-茚-2,1-二亚甲基))二丙二腈(IDIC))对于推动聚合物太阳能电池的发展起着至关重要的作用. 相似文献
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《有机化学》2021,(5)
合成了一系列新型的3-(吲哚-3-基)-4-(吡唑并[3,4-c]哒嗪-3-基)马来酰亚胺,并评价了其对异柠檬酸脱氢酶1突变体(R132H)的抑制活性.大多数化合物对IDH1-R132H表现出较强的活性.其中化合物3-(1-(3-(1-(1H-咪唑-1-基)丙基)-6-溴-1H-吲哚-3-基)-4-(1-甲基-1H-吡唑并[3,4-c]哒嗪-3-基)-1H-吡咯-2,5-二酮(9b)是最有前途的IDH1-R132H抑制剂,IC50值为31 nmol/L,并能显著抑制异柠檬酸脱氢酶1突变(R132H)型人脑星形胶质母细胞瘤细胞中2-HG的产生.根据实验数据进行了初步的构效关系讨论和分子模拟研究. 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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《Analytical letters》2012,45(5):381-386
Abstract Rapid spot analysis of three aminopyrazol derivatives is described: 1-β-(pyridyl-4) -ethyl -3 -methyl-5 -aminopyrazol dichloride (I) 1-isopropyl-3-methyl-5-aminopyrazol (II), and 1-isopropyl-3-ethyl-4-methyl-5-aminopyrazol (III). Sensitivity, maximum dilution and analytical procedure is presented. 相似文献
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Acetals and ketals are a kind of the important compounds and used to protect carbonyl,middle material of the organic synthesis. What's more, they are a sort of the widely use flavor substance. 4-Methyl-2-isopropyl-1,3-dioxolane has fresh fruit odor and apple note. It is used to producing many sorts of essence. And the conventional method to synthesize 4-methyl-2-isopropyl-1,3-dioxolane makes use of sulfuric acid as catalyst in factories. But it causes many problems, such as the erosion of production equipment, difficulty after-treatment, low quality of the products, etc. HPA and its salts shows excellent catalytic activity to the esterification and have recently attracted much attention as catalysts for various industrial processes, because their acidic and redox properties can be controlled at atomic/molecular levels. Misono, Pope [1], and Wang [2]have reviewed the homogeneous catalysis and fine organic synthesis catalyzed by heteropoly compounds. However, there is no report on the synthesis of 4-methyl-2-isopropyl-1,3-dioxolane catalyzed by TiSiW12O40/TiO2. TiSiW12O40/TiO2 was prepared according to reference [3] and identified by means of IR and XRD. The reaction was carried out in a three-neck flask equipped with a stirrer, a reflux condenser, and a thermometer. A certain amounts of isobutyraldehyde,1,2-propanediol and the catalyst was heated to boiling and refluxed until no water flowed off. The purified product was analyzed by IR spectra and 1HNMR.In this paper, we report 4-methyl-2-isopropyl-1,3-dioxolane was synthesized from isobutyraldehyde and 1,2-propanediol in the presence of TiSiW12O40/TiO2. The factors influencing the yield of product and the optimum reaction conditions were discussed. The optimum conditions are molar ratio of isobutyraldehyde to 1,2-propanediol was 1:1.5, the quantity of catalyst was equal to 0.5% feed stock, and the reaction time was 1.0 h. TiSiW12O40/TiO2 was an excellent catalyst to synthesize 4-methyl-2-isopropyl-1,3-dioxolane and the yield can be up to 92.1%. IR spectra of 4-methyl-2-isopropyl- 1,3-dioxolane shows peaks at 1191,1100,1022,950 cm-1; 1HNMR (δH, ppm):4.65-4.67 (d, 1H, CH), 4.02-4.20 (m, 1H, CH), 3.81-3.92 (d, 1H, CH), 3.35-3.43 (t, 1H, CH),1.61~1.85 (m, 1H, CH), 1.14-1.29 (d, 3H, CH3), 0.96 (m, 6H, CH3); nD20=1.4135; b.p. 127-130 ℃.And we found that the catalyst can be utilized repeatedly, moreover, the catalytic activities of the catalyst are almost unchanged after it has been used five times. From the above results and discussion, we can see that the synthesis of 4-methyl-2-isopropyl-1,3-dioxolane catalyzed by TiSiW12O40/TiO2 instead of sulfuric acid has a great prospect of application. 相似文献
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Twelve novel constituents isolated from Burley tobacco condensate by semi-preparative GLC. have been identified as (E)-3,4-epoxy-5-isopropyl-nonane-2,8-dione ( A ), exo-(1-methyl-4-isopropyl-7,8-dioxabicyclo[3.2.1]oct-6-yl)methyl ketone ( B ), exo-1-(1-methyl-4-isopropyl-7,8-dioxabicyclo[3.2.1]oct-6-yl)-ethanol ( C ), (E)-5-isopropyl-8-hydroxy-8-methyl-non-6-en-2-one ( D ), (E)-5-isopropyl-6,7-epoxy-8-hydroxy-8-methyl-nonan-2-one ( E ), endo-2-(1-methyl-4-isopropyl-7,8-dioxabicyclo[3.2.1]oct-6-yl)-propan-2-ol ( F ), 3,3,5-trimethyl-8-isopropyl-4,9-dioxabicyclo[3.3.1]nonan-2-ol ( G ), (E)-5-isopropyl-non-3-ene-2,8-diol ( H ), 5-isopropyl-nonane-2,8-diol ( I ), (E)-5-isopropyl-8-hydroxy-non-6-en-2-one ( J ), 5-isopropyl-8-hydroxy-nonan-2-one ( K ), and (E)-3-isopropyl-6-methyl-hepta-4,6-dien-1-ol ( L ). Compounds A–K were synthesized from norsolanadione ( 2 ), and compound L from 2-isopropyl-5-oxo-hexanal ( 15 ). The relative configuration of the bicyclic internal acetals B, C, F, G and their δ-keto-epoxide precursors A and E is discussed. All these Burley tobacco flavour components belong to a growing family of metabolites structurally related to solanone ( 1 ). They are believed to arise from the breakdown of cembrene-type precursors. 相似文献
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Z.F. Akbalina N.N. Kabalnova S.S. Zlotsky I.A. Grigoriev V.V. Shereshovets G.A. Tolstikov 《Reaction Kinetics and Catalysis Letters》2001,72(1):147-152
The catalytic effect of 2,2,5,5-tetramethyl-4-phenyl-3-imidazoline-3-oxide-1-oxyl on the oxidation of 2-isopropyl-1,3-dioxolane, 2-phenyl-1,3-dioxolane, 2-phenyl-4-chlormethyl-1,3-dioxolane, 2-isopropyl-1,3-dioxane, 2-isopropyl-4-methyl-1,3-dioxane, 2-phenyl-1,3-dioxane, 2-phenyl-4-methyl-1,3-dioxane with oxone and potassium persulfate is reported. The corresponding glycol monoesters were obtained with yields of 90-100%. 相似文献
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The catalytic activities of SO42-/TiO2-MoO3 in synthesizing cyclohexanone ethylene ketal,cyclohexanone 1,2-propanediol ketal, 2-propyl-1,3-dioxolane, 4-methyl-2-isopropyl-1,3-dioxolane,2-isopropyl-1,3-dioxolane, 4-methyl-2-isopropyl-1,3-dioxolane, butanone ethy-lene ketal and butanone 1,2-propanediol ketal were reported. It has been demonstrated that SO42-/TiO2-MoO3 is an excellent catalyst. Various factors concerned in this reaction have been investigated. The optimum conditions have been found, that is, the molar ratio of aldehyde/ketone to alcohol was 1:1.5 or 1:1.3,the mass ratio of the catalyst used to the reactants was 0.25~1.5%, and the reaction time was 45~60 min. Under this conditions, the yield of cyclohexanone ethylene ketal is 82.7%, cyclohexanone 1,2-propanediol ketal is 83.4%, the yield of 2-propyl-1,3-dioxolane is 68.1%,4-methyl-2-isopropyl-1,3-dioxolane is 87.5%, the yield of 2-isopropyl-1,3-dioxolane is 70.7%,4-methyl-2-isopropyl-1,3-dioxolane is 82.5%, the yield of butanone ethylene ketal is 74.1%, and butanone 1,2-propanediol ketal is 94.9%.Some equation and experiment results concerned of the synthetic acetals or ketals were listed as follows. 相似文献
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T. V. Mezhenkova V. R. Sinyakov V. M. Karpov V. E. Platonov 《Russian Journal of Organic Chemistry》2013,49(10):1454-1465
Perfluorinated 1-ethyl-2-methyl- and 1-isopropyl-2-methyl-1,2-dihydrocyclobutabenzenes reacted with pentafluorobenzene in SbF5 to generate perfluoro(1-ethyl-2-methyl-2-phenyl- and perfluoro(1-izopropyl-2-methyl-2-phenyl-1,2-dihydrocyclobutabenzen-1-yl) cations. These cations in SbF5 at 20°C underwent opening of the four-membered ring and its expansion to five-membered. After hydrolysis, perfluorinated 4-[1-(2-propylphenyl)ethylidene]- and 4-[1-(2-isobutylphenyl)ethylidene]-2,5-cyclohexadien-1-ones were obtained together with perfluoro(3-ethyl- and perfluoro(3-isopropyl-2-phenylinden-1-ones). 相似文献
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A method for determining 2-methoxypyrazine, 3-methyl-, 3-ethyl-, 3-isopropyl-, 3-sec.-butyl- and 3-isobutyl-2-methoxypyrazine in musts is described. It involves headspace solid-phase microextraction (SPME) and determination by capillary gas chromatography using nitrogen–phosphorous detection. Pyrazines were satisfactorily separated under isothermal conditions, and quantification was carried out using 3-isopropyl-2-ethoxypyrazine as the internal standard. Ionic strength, time and temperature were studied in order to make SPME as efficient as possible. The developed method enabled detection limits at the 0.1 ng l−1 levels for some of the analytes. The method was successfully applied to identify and quantify different 3-alkyl-2-methoxypyrazines in experimental musts of Cabernet Sauvignon and Merlot. Their evolution during the ripening was also monitored. 相似文献
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《Journal of organometallic chemistry》2006,691(12):2623-2630
New chiral N,N-bidentate ligands derived from substituted 2-(4-isopropyl-4-methyl-4,5-dihydro-1H-imidazol-5-one-2-yl)pyridines have been prepared and characterised by means of 1H, 13C NMR spectroscopy and optical rotation. Their Cu(II) complexes were characterized by means of elemental analysis, 1H NMR spectroscopy and MS. By means of X-ray diffraction, molecular geometry of the complex of 2-(1-methyl-4-isopropyl-4-methyl-4,5-dihydro-1H-imidazol-5-one-2-yl)pyridine with copper(II) chloride was determined. The complex exhibits heterochiral dimeric arrangement of two square pyramids with one terminal and one bridge-forming chlorine atoms and two nitrogen atoms in the bases of the pyramids. The tops of these pyramids are formed by the remaining chlorine atoms. The complexes prepared catalyse the Henry reaction with the overall yields of 41-97% and with the maximum enantioselective excess of 19%. 相似文献
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Suzuki M Ohuchi Y Asanuma H Kaneko T Yokomori S Ito C Isobe Y Muramatsu M 《Chemical & pharmaceutical bulletin》2000,48(12):2003-2008
A series of N-azabicycloalkyl-1-alkyl-2-oxo-1,2-dihydro-3-quinolinecarboxamides were synthesized and tested for serotonin 5-HT4 receptor-stimulating effects in the regulation of electrically-evoked contraction in guinea pig muscle. Among them, N-azabicycloalkyl-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c, 9c, 10c, 11c, 12c) exhibited potent serotonin 5-HT4 receptor-stimulating activity. The most potent compound, N-(endo-8-methyl-8-azabicyclo[3.2.1 oct-3-yl)-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c, ED50 = 36.3 nMi), was seven times as active as cisapride, while 8c had no affinity for 5-HT1A, 5-HT1D, D2, muscarinic M2 or muscarinic M3 receptors even at 10 microM. Compound 8c stimulated digestive tract motility in conscious fed dogs (1.0 mg/kg p.o.). 相似文献
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Summary A systematic study was made of the catalytic dehydration of 4-methyl-1-penten-3-ol (Ia), 3,4-dimethyl-1--penten-3-ol (Ib), 3-isopropyl-4-methyl-1-penten-3-ol (Ic), 2-methyl-4-penten-2-ol (II), 2-methyl-3-penten-2-ol (III), 4-methyl-3-penten-2-ol (IV), and 2-methyl-4-hexen-3-ol (V). In the course of this study methods were developed for the preparation of the following substituted gem-dimethylbutadienes: 4-methyl-1,3-pentadiene (VIII), 3,4-dimethyl-1,3-pentadiene (IX), 2-methyl-2,4-hexadiene (XI), and 3-isopropyl-4-methyl-1,3-pentadiene (XIV). 相似文献