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.
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.
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.
, 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.
