37542-78-2Relevant academic research and scientific papers
Palladium(II) supported on polycarbosilane: Application as reusable catalyst for Heck reaction
Mangala, Kunniyur,Sinija,Sreekumar, Krishnapillai
, p. 87 - 92 (2015)
Heck reaction catalyzed by palladium(II) attached polycarbosilane is reported. Polycarbosilane (PCS), which is an organic-inorganic hybrid polymer containing both Si and C in its back bone structure, was synthesized by the polycondensation of trichloromethylsilane and trimethoxyvinylsilane in the presence of sodium metal. Palladium acetate was attached to the polycarbosilane (Pd-PCS) and its catalytic activity was investigated. Heck reaction in which C-C coupling between aryl halides or vinyl halides and activated alkenes in the presence of a base has been selected for the study. Palladium ions supported on PCS have been used as a catalyst for the first time and it efficiently catalyzed Heck reaction and an yield of 75-90% was obtained with different substrates. For comparison, catalytic activities of Pd ions supported on SBA-15, activated charcoal and amorphous silica were also investigated. Results indicate the superior activity of Pd-PCS.
Discovery of a novel inhibitor of nitric oxide production with potential therapeutic effect on acute inflammation
Zhu, Long-Qing,Fan, Xiao-Hong,Li, Jun-Fang,Chen, Jin-Hong,Liang, Yan,Hu, Xiao-Ling,Ma, Shu-Meng,Hao, Xiang-Yong,Shi, Tao,Wang, Zhen
supporting information, (2021/05/26)
Inflammation as a host's excessive immune response to stimulation, is involved in the development of numerous diseases. To discover novel anti-inflammatory agents and based on our previous synthetic work on marine natural product Chrysamide B, it and a series of derivatives were synthesized and evaluated for their anti-inflammatory activity on inhibition of LPS-induced NO production. Then the preliminary structure–activity relationships were conducted. Among them, Chrysamide B is the most potent anti-inflammatory agent with low cytotoxicity and strong inhibition on the production of NO (IC50 = 0.010 μM) and the activity of iNOS (IC50 = 0.082 μM) in LPS-stimulated RAW 264.7 cells. Primary studies suggested that the mechanism of action may be that it interfered the formation of active dimeric iNOS but not affected transcription and translation. Furthermore, its good performance of anti-inflammatory effect on LPS-induced multiple inflammatory cytokines production, carrageenan-induced paw edema, and endotoxin-induced septic mice, was observed. We believe that these findings would provide an idea for the further modification and research of these analogs in the future.
Palladium Loaded Dendronized Polymer as Efficient Polymeric Sustainable Catalyst for Heck Coupling Reaction
Hiba, K.,Krishna, G. Anjali,Prathapan, S.,Sreekumar, K.
, (2021/08/18)
The palladium incorporated amine-functionalized dendronized polymer was synthesized by the addition of palladium acetate to dendronized polymer in methanol at room temperature. Palladium species are immobilized onto the dendritic structure by their coordination with amino functional groups. The newly developed dendritic system showed high palladium content in the low generation level itself, which was found to be 4.19?mmol/g. This was fairly higher than, the other palladium-based catalysts. Energy dispersive X-ray spectroscopy, Fourier transform infrared spectroscopy, UV–Visible spectroscopy, and X-ray photoelectron spectroscopy were used to confirm the successful synthesis of the new catalyst. It was used as a homogeneous palladium catalyst for Heck coupling reaction between olefins and differently substituted aryl halides and the products were isolated in high yield. The products isolated were in trans configuration, which indicated the selectivity of the newly developed catalytic system. Also, this catalyst system was reused up to nine times without a significant decrease in its catalytic activity. The easy accessibility of catalytic sites, stability, resistance to metal leaching, high catalytic activity and remarkable stereoselectivity with a low amount of catalyst are all due to the dendritic support. The docking study was carried out for all the stilbene derivatives obtained by the Heck coupling reaction against DprE1 protein to study its potential antitubercular activity. All the compounds displayed superior docking score values over the range ??6.5 to ??8.2?kcal/mol, compared to the standard drug isoniazid with docking score of ??6.1?kcal/mol against DprE1. Graphic Abstract: [Figure not available: see fulltext.]
Novel piperazine compound as well as preparation method and application thereof
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Paragraph 0060-0064, (2020/04/22)
The structural general formula of a novel piperazine compound is shown in the specification. The invention aims to provide a novel anti-inflammatory drug with high efficiency and low side effect. Because typical marine characteristic skeleton molecules ri
Selective preparation of functionalized dienes from allylic phosphonium salts through the wittig reaction
Sa, Marcus M.,Meier, Lidiane
, p. 384 - 391 (2013/09/23)
A convenient and general method for the synthesis of stereochemically defined dienes from allylic phosphonium salts under simple conditions is described. Selective preparation of trisubstituted dienes was performed with good-to-excellent yields in mild ba
Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV)
Beaulieu, Pierre L.,Boes, Michael,Cordingley, Michael G.,Chabot, Catherine,Fazal, Gulrez,Garneau, Michel,Gillard, James R.,Jolicoeur, Eric,Laplante, Steven,McKercher, Ginette,Poirier, Martin,Poupart, Marc-Andre,Tsantrizos, Youla S.,Duan, Jianmin,Kukolj, George
, p. 7650 - 7666,17 (2020/08/24)
Combinations of direct acting antivirals (DAAs) that have the potential to suppress emergence of resistant virus and that can be used in interferon-sparing regimens represent a preferred option for the treatment of chronic HCV infection. We have discovered allosteric (thumb pocket 1) non-nucleoside inhibitors of HCV NS5B polymerase that inhibit replication in replicon systems. Herein, we report the late-stage optimization of indole-based inhibitors, which began with the identification of a metabolic liability common to many previously reported inhibitors in this series. By use of parallel synthesis techniques, a sparse matrix of inhibitors was generated that provided a collection of inhibitors satisfying potency criteria and displaying improved in vitro ADME profiles. "Cassette" screening for oral absorption in rat provided a short list of potential development candidates. Further evaluation led to the discovery of the first thumb pocket 1 NS5B inhibitor (BILB 1941) that demonstrated antiviral activity in patients chronically infected with genotype 1 HCV.
Microwave-assisted synthesis of the (E)-α-methylalkenoate framework from multifunctionalized allylic phosphonium salts
Meier, Lidiane,Ferreira, Misael,Sa, Marcus M.
, p. 179 - 186 (2012/07/14)
A convenient and general microwave-assisted method for the synthesis of stereochemically defined α-methylalkenoic acids and esters from allylic phosphonium salts in a basic aqueous medium is described. A selective preparation of acids or esters was dependent on the base (NaOH or NaHCO 3) employed in the reaction and could be achieved with good to excellent yields under mild conditions in the absence of hydrides and reducing agents.
