- Efficient and sustainable laccase-catalyzed iodination of: P -substituted phenols using KI as iodine source and aerial O2 as oxidant
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The laccase-catalyzed iodination of p-hydroxyarylcarbonyl- and p-hydroxyarylcarboxylic acid derivatives using KI as iodine source and aerial oxygen as the oxidant delivers the corresponding iodophenols in a highly efficient and sustainable manner with yields up to 93% on a preparative scale under mild reaction conditions.
- Sdahl, Mark,Conrad, Jürgen,Braunberger, Christina,Beifuss, Uwe
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p. 19549 - 19559
(2019/07/05)
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- Highly Stereoselective Synthesis of trans -Dihydronarciclasine Analogues
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Several new trans -dihydronarciclasine analogues were stereo selectively synthesised by applying our feasible and efficient process developed recently. These new phenanthridone alkaloid derivatives were obtained in both racemic and optically active forms. During their enantioselective syntheses, high selectivities (up to 99% ee) were achieved by using (8 S,9 S)-9-amino(9-deoxy)epiquinine as an organocatalyst. The modifications, the introduction of ethoxy or methoxy groups, were made in ring A of the phenanthridone scaffold.
- Varró, Gábor,Mattyasovszky, Lenke,Grün, Alajos,Simon, András,Hegedüs, László,Kádas, István
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p. 625 - 643
(2017/11/27)
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- Novel aminotetrazole derivatives as selective STAT3 non-peptide inhibitors
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The development of inhibitors blocking STAT3 transcriptional activity is a promising therapeutic approach against cancer and inflammatory diseases. In this context, the selectivity of inhibitors against the STAT1 transcription factor is crucial as STAT3 and STAT1 play opposite roles in the apoptosis of tumor cells and polarization of the immune response. A structure-based virtual screening followed by a luciferase-containing promoter assay on STAT3 and STAT1 signaling were used to identify a selective STAT3 inhibitor. An important role of the aminotetrazole group in modulating STAT3 and STAT1 inhibitory activities has been established. Optimization of the hit compound leads to 23. This compound inhibits growth and survival of cells with STAT3 signaling pathway while displaying a minimal effect on STAT1 signaling. Moreover, it prevents lymphocyte T polarization into Th17 and Treg without affecting their differentiation into Th1 lymphocyte.
- Pallandre, Jean-René,Borg, Christophe,Rognan, Didier,Boibessot, Thibault,Luzet, Vincent,Yesylevskyy, Semen,Ramseyer, Christophe,Pudlo, Marc
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supporting information
p. 163 - 174
(2015/09/21)
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- SPIRO AZETIDINE ISOXAZOLE DERIVATIVES AND THEIR USE AS SSTR5 ANTAGONISTS
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Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
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Paragraph 0515
(2014/09/29)
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- NAPHTHALENE DERIVATIVE
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The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
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Paragraph 0652
(2013/06/27)
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- WOOD PROTECTION AGAINST MICROORGANISMS BY LACCASE-CATALYSED IODINATION
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A method for protecting a phenolic substances comprising material like wood against vermins, in particular microorganisms, comprises treating said phenolic substances comprising material with iodide in the presence of laccase, in particular with a liquid composition comprising iodide and laccase. Materials like wood treated by this method can be used as such or - if in form of small pieces like shavings or wood flour - together with a binder for protective coatings and/or laminates like antibacterial wood fibre plates, inner or outer panelling, wallpapers, and packagings.
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Page/Page column 27
(2014/01/07)
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- A practical iodination of aromatic compounds by using iodine and iodic acid
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This article describes simple and efficient method for the iodination of different aromatic amines, hydroxy aromatic aldehydes, hydroxy acetophenones and phenols using iodine and iodic acid in ethanol as a solvent. Notable advantages include mild reaction condition, no need of catalyst, short reaction time, simple practical procedure, giving excellent yield of the product. Copyright Taylor & Francis Group, LLC.
- Shinde, Avinash T.,Zangade, Sainath B.,Chavan, Shivaji B.,Vibhute, Archana Y.,Nalwar, Yogesh S.,Vibhute, Yeshwant B.
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experimental part
p. 3506 - 3513
(2011/02/22)
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