- Nitrogen-Centered Concave Molecules with Double Fused Pentagons
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Distinctive concave compounds bearing a nitrogen core and double fused pentagons were synthesized with a palladium-catalyzed intramolecular coupling of 1-chloro-8H-indolo[3,2,1-de]acridine as the key step. Structural analysis confirmed the formation of bo
- Deng, Niping,Zhang, Gang
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- Embedding Heteroatoms and Adjacent Pentagons in Concave Molecules
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Bowl-shaped molecules, which can be viewed as fragments of fullerenes, have been extensively studied owing to their interesting fundamental properties derived from their unique geometry, and the possibilities for their further functionalization, with pote
- Zhang, Gang
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Read Online
- Catalytic Oxidative Coupling Cyclization for Construction of Benzofuroindolenines under Mild Reaction Conditions
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We describe iron-catalyzed oxidative coupling cyclization of tetrahydrocarbazoles or THβCs or THγCs to form benzofuroindolenines as fused polycyclic indoles. This mild, efficient and simple approach afforded a library of more than 52 complex compounds across a range of substrate classes with good to excellent yields. (Figure presented.).
- Lin, Yuqi,Ye, Jinxiang,Zhang, Wenting,Gao, Yu,Chen, Haijun
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supporting information
p. 432 - 435
(2018/12/13)
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- Method for preparing indole compounds through catalysis of ionic liquid
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The invention relates to a green synthesis method of one type of indole derivatives. The method is characterized by taking sulfonic acid ionic liquid as a catalyst, taking aliphatic ketone, aromatic ketone and aromatic hydrazine hydrochloride as raw materials, reacting in water, filtering and drying a reaction mixture to obtain indole compounds. The method is simple to operate; the raw materials are low intoxicity and low in costs; the reaction condition is mild; the product is easy to separate; the synthesis process is environmentally-friendly; the indole compounds are high in purity; the catalyst can be directly reused without treatment; the method is green and environmentally-friendly, and is suitable for industrial production.
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Paragraph 0046-0048
(2018/02/04)
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- Discovery of lead compounds targeting the bacterial sliding clamp using a fragment-based approach
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The bacterial sliding clamp (SC), also known as the DNA polymerase III β subunit, is an emerging antibacterial target that plays a central role in DNA replication, serving as a protein-protein interaction hub with a common binding pocket to recognize linear motifs in the partner proteins. Here, fragment-based screening using X-ray crystallography produced four hits bound in the linear-motif-binding pocket of the Escherichia coli SC. Compounds structurally related to the hits were identified that inhibited the E. coli SC and SC-mediated DNA replication in vitro. A tetrahydrocarbazole derivative emerged as a promising lead whose methyl and ethyl ester prodrug forms showed minimum inhibitory concentrations in the range of 21-43 μg/mL against representative Gram-negative and Gram-positive bacteria species. The work demonstrates the utility of a fragment-based approach for identifying bacterial sliding clamp inhibitors as lead compounds with broad-spectrum antibacterial activity.
- Yin, Zhou,Whittell, Louise R.,Wang, Yao,Jergic, Slobodan,Liu, Michael,Harry, Elizabeth J.,Dixon, Nicholas E.,Beck, Jennifer L.,Kelso, Michael J.,Oakley, Aaron J.
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supporting information
p. 2799 - 2806
(2014/04/17)
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- Novel SO3H-functionalized ionic liquids catalyzed a simple, green and efficient procedure for Fischer indole synthesis in water under microwave irradiation
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Novel SO3H-functionalized ionic liquids were successfully applied as catalysts for one-pot Fischer indole synthesis under microwave irradiation and in a water medium. Various types of indoles were prepared using single-carbonyl ketones/aldehydes or cyclohexandiones with aryhydrazine hydrochlorides in 86-96% yields in water under microwave irradiation. The indole products could be conveniently separated from the reaction mixture through filtration, and the catalytic system of [(HSO3-p)2im] [CF3SO3]/H2O could be reused directly without any treatment. The entire process is simple, time saving, and environmentally friendly.
- Li, Bai Lin,Zhong, Ai Guo,Xu, Dan-Qian
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p. 45 - 50,6
(2020/10/15)
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- A microwave-assisted, propylphosphonic anhydride (T3P) mediated one-pot Fischer indole synthesis
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A rapid, mild, and high yielding protocol for the Fischer indolization of arylhydrazines with T3P under microwave irradiation is described. Significant features of this method include short reaction times and preparative ease.
- Desroses, Matthieu,Wieckowski, Krzysztof,Stevens, Marc,Odell, Luke R.
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supporting information; experimental part
p. 4417 - 4420
(2011/09/19)
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- Fischer indole synthesis catalyzed by novel SO3H-functionalized ionic liquids in water
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Novel SO3H-functionalized ionic liquids bearing two alkyl sulfonic acid groups in the imidazolium cations were designed and successfully applied as catalysts for the one-pot Fischer indole synthesis in water medium. The sequence of the catalytic activity observed in the transformation was in good agreement with the Bronsted acidity order determined by the Hammett method. Various types of indoles from single-carbonyl ketones/aldehydes and cyclohexandiones were provided in 68-96% yields using the catalytic system of [(HSO3-p)2im][HSO4]/H2O. The indole products could be conveniently separated from the reaction mixture by filtration and the dissolved catalyst could be regenerated by treatment with a strongly acidic cation exchange resin, which meant the whole process was performed in water without using any organic solvents.
- Xu, Dan-Qian,Wu, Jian,Luo, Shu-Ping,Zhang, Ji-Xu,Wu, Jia-Yi,Du, Xiao-Hua,Xu, Zhen-Yuan
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supporting information; experimental part
p. 1239 - 1246
(2010/04/26)
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- HEPATITIS C VIRUS ENTRY INHIBITORS
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The present invention relates to the use of tricyclic diphenylamine derivative compounds for prevention and/or treatment of Hepatitis C virus (HCV) infection by inhibiting HCV entry into permissive cells.
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Page/Page column 67
(2010/11/30)
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- One-pot synthesis of polysubstituted indoles from aliphatic nitro compounds under mild conditions
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Polysubstituted indoles can be prepared directly from functionalized nitroalkanes under very mildly acidic conditions in a simple, one-pot, two-stage procedure.
- Simoneau, Christopher A.,Strohl, Alexis M.,Ganem, Bruce
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p. 1809 - 1811
(2008/02/05)
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- Microwave-assisted one-pot synthesis of 1,2,3,4-tetrahydrocarbazoles
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A series of 1,2,3,4-tetrahydrocarbazoles 3a-m were synthesized by the reaction of substituted 2-bromocyclohexanones 2a-c with appropriate anilines 1a-i under microwave irradiation without any other catalysts. Copyright Taylor & Francis Group, LLC.
- Chen, Jing,Hu, Yongzhou
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p. 1485 - 1494
(2007/10/03)
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- Ruthenium Complex Catalyzed N-Heterocyclization. Syntheses of Quinolines and Indole Derivatives from Aminoarenes and 1,3-Propanediol of Glycols
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Aniline reacts with 1,3-propanediol under reflux in diglyme with spontaneous hydrogen evolution in the presence of a catalytic amount of ruth enium trichloride hydrate ( RuCl3*nH2O)-tributylphosphine (PBu3) to give quinoline in good yield.The yield of quinoline was markedly affected by the molar ratios of aniline to 1,3-propanediol and PBu3 to RuCl3*nH2O.The best yield (76percent) was achieved at the molar ratios of 2.5 of aniline / 1,3-propanediol and 2.0 of PBu3 / RuCl3*nH2O.Also, N-substituted anilines react with ethylene glycol in the presence of a catalytic amount of dichlor otris(triphenylphosphine)ruthenium (RuCl2(PPh3)3) to give N-substituted indole derivatives.The reactions were carried out at 180 deg C in dioxane with spontaneus hydrogen evolution.Aminoarenes also react with 2,3-butanediol and 1,2-cyclohexanediol ( mixture of cis and trans ) in the presence of RuCl2(PPh3)3 to give the corresponding 2,3-dimethylindoles and 1,2,3,4-tetrahydrocarbazoles in good to excellent yields.As the key intermediates of the reactions, N,N'-diarylpropylenediamine (5a) and N,N'-diarylethylenediamine (5b) and their dehydrogenated imine derivatives are postulated.
- Tsuji, Yasushi,Huh, Keun-Tae,Watanabe, Yoshihisa
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p. 1673 - 1680
(2007/10/02)
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- Process for preparing indole derivatives
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Certain indole derivatives, and especially certain 1,2,3,4-tetrahydrocarbazoles, 1,2,3,4-tetrahydro-γ-carbolines and 1,2,3,4-tetrahydropyrrolo-[3,4-b]indoles are prepared by reacting the appropriate phenylhydrazine salt and ketone in the presence of a weakly basic solvent such as pyridine, quinoline, N,N-dimethylaniline, picoline or lutidine at a temperature in the range of about 50° to 180° C.
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