27007-53-0Relevant articles and documents
2, 4, 7-trisubstituted fluorene compound and electronic device thereof
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Paragraph 0127, (2021/02/20)
The invention provides a 2, 4, 7-trisubstituted fluorene compound and an electronic device thereof. According to the 2, 4, 7-trisubstituted fluorene compound disclosed by the invention, a fluorene rigid structure is introduced, so that the 2, 4, 7-trisubstituted fluorene compound is excellent in film-forming property and thermal stability, and can be used for preparing an organic light-emitting device, an organic field effect transistor and an organic solar cell. In addition, the 2, 4, 7-trisubstituted fluorene compound can be used as a constituent material of a hole injection layer, a hole transport layer, a light emitting layer, an electron blocking layer, a hole blocking layer or an electron transport layer, and can reduce driving voltage, improve efficiency and brightness, prolong theservice life and the like. The preparation method of the 2, 4, 7-trisubstituted fluorene compound is simple, raw materials are easy to obtain, and industrial development requirements can be met.
Palladium/Acid Relay Catalyzed Tandem Heck Coupling/6-Endo Cyclization between ortho-Halogenated Benzoates and Unactivated Terminal Alkenes for the Synthesis of 1-Isochromanones
Wen, Zhen-Kang,Ge, Xiao-Min,Zhao, Ze-Kai,Chao, Jian-Bin
supporting information, p. 983 - 988 (2019/01/30)
We report a unique and expeditious route to synthesize 1-isochromanone derivatives through palladium catalyzed tandem Heck coupling/6-endo hydroacyloxylation cyclization between readily available ortho-halogenated benzoates and unactivated alkenes. Various 2-bromo or 2-iodo benzoates can be coupled efficiently with a broad range of alkenes to afford functionalized 1-isochromanones in high yields. Significantly, this cost-efficient and easy-to-handle synthetic methodology will have great prospect application in the synthetic and medicinal chemistry. (Figure presented.).
Vitamin Catalysis: Direct, Photocatalytic Synthesis of Benzocoumarins via (-)-Riboflavin-Mediated Electron Transfer
Morack, Tobias,Metternich, Jan B.,Gilmour, Ryan
supporting information, p. 1316 - 1319 (2018/03/09)
An operationally simple protocol is disclosed to facilitate entry to benzo-3,4-coumarins directly from biaryl carboxylic acids without the need for substrate prefunctionalization. Complementary to classic lactonization strategies, this disconnection relies on the oxidation competence of photoactivated (-)-riboflavin (vitamin B2) to generate the heterocyclic core via photoinduced single electron transfer. Collectively, the inexpensive nature of the catalyst, ease of execution, and absence of external metal additives are a convincing endorsement for the incorporation of simple vitamins in contemporary catalysis.
Divergent syntheses of iodinated isobenzofuranones and isochromenones by iodolactonization of 2-alkynylbenzoic acids in ionic liquids
Mancuso, Raffaella,Pomelli, Christian C.,Malafronte, Francesco,Maner, Asif,Marino, Nadia,Chiappe, Cinzia,Gabriele, Bartolo
supporting information, p. 4831 - 4841 (2017/07/10)
The regiochemical outcome of the iodolactonization of 2-alkynylbenzoic acids, carried out at 100 °C in ionic liquids (ILs) as unconventional solvents and with molecular iodine as the iodine source, in the absence of external bases, was found to be strongl
HALO-SUBSTITUTED PIPERIDINES AS OREXIN RECEPTOR MODULATORS
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Page/Page column 112, (2017/09/05)
The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.
Synthesis and antimicrobial evaluation of amixicile-based inhibitors of the pyruvate-ferredoxin oxidoreductases of anaerobic bacteria and Epsilonproteobacte
Kennedy, Andrew J.,Bruce, Alexandra M.,Gineste, Catherine,Ballard, T. Eric,Olekhnovich, Igor N.,Macdonald, Timothy L.,Hoffman, Paul S.
supporting information, p. 3980 - 3987 (2016/07/11)
Amixicile is a promising derivative of nitazoxanide (an antiparasitic therapeutic) developed to treat systemic infections caused by anaerobic bacteria, anaerobic parasites, and members of the Epsilonproteobacteria (Campylobacter and Helicobacter). Amixicile selectively inhibits pyruvate-ferredoxin oxidoreductase (PFOR) and related enzymes by inhibiting the function of the vitamin B1 cofactor (thiamine pyrophosphate) by a novel mechanism. Here, we interrogate the amixicile scaffold, guided by docking simulations, direct PFOR inhibition assays, and MIC tests against Clostridium difficile, Campylobacter jejuni, and Helicobacter pylori. Docking simulations revealed that the nitro group present in nitazoxanide interacts with the protonated N4′-aminopyrimidine of thiamine pyrophosphate (TPP). The ortho-propylamine on the benzene ring formed an electrostatic interaction with an aspartic acid moiety (B456) of PFOR that correlated with improved PFOR-inhibitory activity and potency by MIC tests. Aryl substitution with electron-withdrawing groups and substitutions of the propylamine with other alkyl amines or nitrogen-containing heterocycles both improved PFOR inhibition and, in many cases, biological activity against C. difficile. Docking simulation results correlate well with mechanistic enzymology and nuclear magnetic resonance (NMR) studies that show members of this class of antimicrobials to be specific inhibitors of vitamin B1 function by proton abstraction, which is both novel and likely to limit mutation-based drug resistance.
Formation of substituted 1-naphthols and related products via dimerization of alkyl 3-(o-halo(het)aryl)-oxopropanoates based on a CuI-catalyzed domino C-arylation/condensation/aromatization process
Weischedel, Heike,Sudheendran, Kavitha,Mikhael, Alevtina,Conrad, Jürgen,Frey, Wolfgang,Beifuss, Uwe
, p. 3454 - 3467 (2016/06/06)
Substrates bearing both a β-ketoester moiety and a (het)aryl halide structure element were dimerized to 1-naphthols and related products in the presence of catalytic amounts of CuI in isopropanol. The reaction starts with an intermolecular C-arylation, which is followed by an intramolecular condensation. The final aromatization delivers the highly substituted products with yields up to 81%.
Alkene Dioxygenation with Malonoyl Peroxides: Synthesis of γ-Lactones, Isobenzofuranones, and Tetrahydrofurans
Alamillo-Ferrer, Carla,Karabourniotis-Sotti, Marianna,Kennedy, Alan R.,Campbell, Matthew,Tomkinson, Nicholas C. O.
supporting information, p. 3102 - 3105 (2016/07/13)
Treatment of homoallylic alcohols or carboxylic acids with malonoyl peroxide 1 provides a stereoselective method for the preparation of tetrahydrofurans, γ-lactones, and isobenzofuranones in 44-82% yield and up to 27:1 trans selectivity. Application of this simple and effective heterocyclization in the synthesis of the antidepressant citalopram is also described.
4,4-DIFLUORO-PIPERIDINE-COMPOUNDS
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Paragraph 0271; 0272; 0273, (2015/02/25)
The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N,
PYRROLIDINE THROMBIN INHIBITORS
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Page/Page column 24, (2014/03/21)
Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein R is a heterocycle or -(CR4R5)1-2NH2 , wherein R4 and R5,