51605-97-1Relevant articles and documents
Novel phenylcarbazole type organic compounds and an organic electroluminescent device comprising the same
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Paragraph 0249-0252, (2021/06/09)
An organic compound represented by chemical formula 1 and an organic light emitting device including the same are provided. Chemical Formula 1.
Environmentally benign indole-catalyzed position-selective halogenation of thioarenes and other aromatics
Shi, Yao,Ke, Zhihai,Yeung, Ying-Yeung
supporting information, p. 4448 - 4452 (2018/10/17)
Halogenated aromatic compounds are the cores of many pharmaceutical, agricultural and chemical products but they are commonly prepared using electrophilic halogenation reactions in non-green chlorinated solvents under harsh conditions. A separate problem happens in the aromatic halogenation of thioarenes because they readily undergo oxidative side-reactions. Herein we report an environmentally benign electrophilic bromination of aromatics using an indole-catalytic protocol, which is suitable for a wide range of substrates including thioarenes.
INDANYL COMPOUNDS AS VOLTAGE GATED SODIUM CHANNEL MODULATORS
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Page/Page column 63, (2018/09/28)
The invention relates to indanyl compounds, their pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising the same for the treatment, management and /or lessening severity of diseases, disorders, syndromes or conditions which are associated with the voltage-gated sodium channels (VGSC). More specifically the present invention provides compounds having the structure of Formula (I).
Copper-Catalyzed Enantioselective Conjugate Addition to α,β-Unsaturated Aldehydes with Various Organometallic Reagents
Goncalves-Contal, Sylvie,Gremaud, Ludovic,Palais, La?titia,Babel, Lucille,Alexakis, Alexandre
, p. 3301 - 3308 (2016/09/12)
β-Substituted aldehydes constitute a very important class of compounds found in nature. Synthesis of this motif can be envisioned by C-C bond formation on enals. For this purpose, we report herein the development of enantioselective copper-catalyzed conjugate addition of various organometallic reagents to α,β-unsaturated aldehydes with (R)-H8BINAP, (R)-TolBINAP, and (R)-SEGPHOS as chiral ligands. Three sets of conditions were successfully developed and several enals were used. Reactivity and regio- and enantioselectivities were strongly dependent on reaction conditions and substrates. Good to excellent regio- and enantioselectivities were obtained with zinc reagents R2Zn and aluminum reagents R3Al. However, the asymmetric conjugate addition of Grignard reagents afforded only moderate to good regio- and enantioselectivities.
Design, synthesis, and biological evaluation of novel transrepression- selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11- methylene-6 H-dibenz[ b, e ]azepin-6-one skeleton
Aoyama, Atsushi,Endo-Umeda, Kaori,Kishida, Kenji,Ohgane, Kenji,Noguchi-Yachide, Tomomi,Aoyama, Hiroshi,Ishikawa, Minoru,Miyachi, Hiroyuki,Makishima, Makoto,Hashimoto, Yuichi
, p. 7360 - 7377 (2012/11/07)
To obtain novel transrepression-selective liver X receptor (LXR) ligands, we adopted a strategy of reducing the transactivational agonistic activity of the 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one derivative 10, which exhibits LXR-mediated transrepressional and transactivational activity. Structural modification of 10 based on the reported X-ray crystal structure of the LXR ligand-binding domain led to a series of compounds, of which almost all exhibited transrepressional activity at 1 or 10 μM but showed no transactivational activity even at 30 μM. Among the compounds obtained, 18 and 22 were confirmed to have LXR-dependent transrepressional activity by using peritoneal macrophages from wild-type and LXR-null mice. A newly developed fluorescence polarization assay indicated that they bind directly to LXRα. Next, further structural modification was performed with the guidance of docking simulations with LXRα, focusing on enhancing the binding of the ligands with LXRα through the introduction of substituents or heteroatom(s). Among the compounds synthesized, compound 48, bearing a hydroxyl group, showed potent, selective, and dose-dependent transrepressional activity.
Enantioselective copper-catalyzed conjugate addition of trimethylaluminium to β,γ-unsaturated α-ketoesters
Gremaud, Ludovic,Alexakis, Alexandre
supporting information; experimental part, p. 794 - 797 (2012/03/09)
Not a cop out: The copper-catalyzed asymmetric conjugate addition of organometallic reagents to Michael acceptors is an important methodology for forming a C-C bond in an enantioselective manner. Such an addition of Me 3Al to β,γ-unsaturated α-
HETEROTRICYCLIC METALLOPROTEASE INHIBITORS
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Page/Page column 63, (2008/12/05)
The present invention relates generally to azatricyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 a
