19235-89-3Relevant articles and documents
Pyridylpyrazole N∧N ligands combined with sulfonyl-functionalised cyclometalating ligands for blue-emitting iridium(III) complexes and solution-processable PhOLEDs
Benjamin, Helen,Fox, Mark A.,Batsanov, Andrei S.,Al-Attar, Hameed A.,Li, Chensen,Ren, Zhongjie,Monkman, Andrew P.,Bryce, Martin R.
, p. 10996 - 11007 (2017)
A series of blue iridium(iii) complexes (12-15) comprising sulfonyl-functionalised phenylpyridyl cyclometalating ligands and pyridylpyrazole N^N ligands are reported, with an X-ray crystal structure obtained for 12. The complexes are highly emissive with photoluminescence quantum yields of 0.52-0.70 in dichloromethane solutions: two of the complexes (12 and 14) show emissions at λPLmax 457 nm which is considerably blue-shifted compared to the archetypal blue emitter FIrpic (λmax 468 nm). The short excited state lifetimes (1.8-3.3 μs) and spectral profiles are consistent with phosphorescence from a mixture of ligand-centred and MLCT excited states. Density functional (DFT) and time dependent DFT (TD-DFT) calculations are in agreement with the electrochemical properties and the blue phosphorescence of the complexes. The additional mesityl substituent on the pyridylpyrazole ligand of 12 and 13 enhances the solubility of the complexes facilitating thin film formation by solution processing. Phosphorescent organic light-emitting diodes (PhOLEDs) have been fabricated using 12 or 13 in a solution-processed single-emitting layer using either poly(vinylcarbazole) (PVK) or 1,3-bis(N-carbazolyl)benzene (mCP) as host. The most blue-shifted electroluminescence (λELmax 460 nm, CIEx,y 0.15, 0.21) is obtained for an OLED containing complex 12 and mCP, with a brightness of 5400 cd m-2 at 10 V which is high for PhOLEDs with similar blue CIE coordinates using a solution-processed emitter layer.
Thiocyanate-free Ru(II) sensitizers with a 4,4′-dicarboxyvinyl-2, 2′-bipyridine anchor for dye-sensitized solar cells
Wu, Kuan-Lin,Ku, Wan-Ping,Wang, Sheng-Wei,Yella, Aswani,Chi, Yun,Liu, Shih-Hung,Chou, Pi-Tai,Nazeeruddin, Mohammad K.,Graetzel, Michael
, p. 2285 - 2294 (2013)
A new class of thiocyanate-free Ru(II) sensitizers with 4,4′-dicarboxyvinyl-2,2′-bipyridine anchor and two trans-oriented pyrid-2-yl pyrazolate (or triazolate) functional chromophores is synthesized, characterized, and evaluated in dye-sensitized solar cells (DSCs). Despite their enhanced red response and absorptivity when compared to the parent sensitizer TFRS-2 that possesses standard 4,4′-dicarboxyl-2,2′-bipyridine anchor and shows the best conversion efficiency of η = 9.82%, the newly synthesized carboxyvinyl-pyrazolate sensitizers, TFRS-11-TFRS-13, exhibit inferior performance characteristics in terms of short-circuit current density (JSC), open-circuit voltage (VOC), and power conversion efficiency (η), the latter being recorded to be in the range 5.60-7.62%. The reduction in device efficiencies is attributed to a combination of poor packing of these sensitizers on the TiO2 surface and less positive ground-state oxidation potentials, which, respectively, increase charge recombination with I3- in electrolytes and impede the regeneration of sensitizers by I- anions. The latter obstacle can be circumvented in part by the replacement of the pyrazolates with triazolates, forming the TFRS-14 sensitizer, which exhibits an improved JSC, VOC, and η of 16.4 mAcm-2, 0.77 V, and 9.02%, respectively. Copyright
Preparation method of 2-cyano-4-fluoropyridine
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, (2021/01/30)
The invention discloses a preparation method of 2-cyano-4-fluoropyridine, which comprises the steps of by using 4-chloropyridine-2-methyl formate as a raw material, carrying out ester ammonolysis reaction, amide dehydration reaction and halogen exchange reaction to prepare the 2-cyano-4-fluoropyridine. The method is simple in synthesis process, mild in reaction condition, high in yield and good inproduct purity; the used raw materials are easy to obtain and low in cost, and the preparation method is suitable for industrial production.
A Transition-Metal-Free One-Pot Cascade Process for Transformation of Primary Alcohols (RCH2OH) to Nitriles (RCN) Mediated by SO2F2
Jiang, Ying,Sun, Bing,Fang, Wan-Yin,Qin, Hua-Li
, p. 3190 - 3194 (2019/05/21)
A new transition-metal-free one-pot cascade process for the direct conversion of alcohols to nitriles was developed without introducing an “additional carbon atom”. This protocol allows transformations of readily available, inexpensive, and abundant alcohols to highly valuable nitriles.
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation
Felts, Andrew S.,Rodriguez, Alice L.,Blobaum, Anna L.,Morrison, Ryan D.,Bates, Brittney S.,Thompson Gray, Analisa,Rook, Jerri M.,Tantawy, Mohammed N.,Byers, Frank W.,Chang, Sichen,Venable, Daryl F.,Luscombe, Vincent B.,Tamagnan, Gilles D.,Niswender, Colleen M.,Daniels, J. Scott,Jones, Carrie K.,Conn, P. Jeffrey,Lindsley, Craig W.,Emmitte, Kyle A.
supporting information, p. 5072 - 5085 (2017/06/28)
Preclinical evidence in support of the potential utility of mGlu5 NAMs for the treatment of a variety of psychiatric and neurodegenerative disorders is extensive, and multiple such molecules have entered clinical trials. Despite some promising results from clinical studies, no small molecule mGlu5 NAM has yet to reach market. Here we present the discovery and evaluation of N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (27, VU0424238), a compound selected for clinical evaluation. Compound 27 is more than 900-fold selective for mGlu5 versus the other mGlu receptors, and binding studies established a Ki value of 4.4 nM at a known allosteric binding site. Compound 27 had a clearance of 19.3 and 15.5 mL/min/kg in rats and cynomolgus monkeys, respectively. Imaging studies using a known mGlu5 PET ligand demonstrated 50% receptor occupancy at an oral dose of 0.8 mg/kg in rats and an intravenous dose of 0.06 mg/kg in baboons.
Design, synthesis and antitumor activities of novel bis-aryl ureas derivatives as Raf kinase inhibitors
Zhan, Wenhu,Li, Yanyang,Huang, Weiping,Zhao, Yanjin,Yao, Zhenglin,Yu, Shanyou,Yuan, Shoujun,Jiang, Falong,Yao, Shan,Li, Shuxin
experimental part, p. 4323 - 4329 (2012/08/28)
A series of novel bis-aryl ureas containing trifluoromethyl imidazolyl group targeting Raf kinase were designed and synthesized based on the lead compound of Sorafenib. All the prepared compounds were evaluated for their in vitro antiproliferative activities against three human cancer cell lines including MDA-MB-231 (breast), BGC-823 (gastric), and SMMC-7721 (liver). Several compounds from the series exhibited excellent antitumor activities against all three tested cancer lines. Further their inhibitory activities against Raf kinase were investigated, and three compounds (11c, 11d, and 11p) demonstrated better activities than contrast drug Sorafenib. Especially compound 11c was found to be a potent and selective Raf kinase inhibitor and could be considered as a candidate compound for further development.
A simple procedure for the preparation of 2-cyano-4-chloropyridines
Veerareddy, Arava,Surendrareddy, Gogireddy,Dubey
experimental part, p. 961 - 964 (2011/09/16)
Figure represented. 4-Nitro-pyridine-N-oxides are reacted with ethylchloroformate and trimethylsilyl cyanide to give 4-chloro-2-cyanopyridine.
AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
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, (2010/01/29)
The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
The synthesis and microbiological activity of new 4-chloropyridin-2-yl derivatives
Bogdanowicz, Agnieszka,Foks, Henryk,Kedzia, Anna,Kwapisz, Ewa,Zwolska, Zofia,Augustynowicz-Kopec, Ewa
experimental part, p. 2217 - 2231 (2010/04/29)
Synthesis of 4-chloropicolinamidrazone derivatives starting from 4-chloropicolinamide is described. The desired compounds were formed by reactions of methyl 4-chloropicolinohydrazonamide or 4-chloro-N′-methylpicolinohydrazonamide with suitable counter partners (carbon disulfide, alkyl halides, aldehydes, ketones, carbohydrazonamides or isothiocyanates) or via 4-chloropicolinimidate, obtained by a convenient method from nitrile with catalytic amount of DBU. Selected products were screened for bacteriostatic and tuberculostatic activity.
Substituted benzimidazoles and methods of preparation
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Page/Page column 43, (2008/06/13)
Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined herein
