- MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.
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- Organometallic complex and Organic light emitting diode comprising the same
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An organometallic complex and an organic light emitting device including the same are disclosed. (by machine translation)
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- A preparation method of 4-tert-butyl-2-chloropyridine and 4-tert-butyl-2,6-dichloro-pyridine
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The invention discloses a preparation method of 4-tert-butyl-2-chloropyridine and 4-tert-butyl-2,6-dichloro-pyridine. 4-tert-butylpyridine is used as a raw material to be reacted with a chlorination reagent at set temperature under the action of a strong base and an additive to obtain the 4-tert-butyl-2-chloropyridine, and the 4-tert-butyl-2-chloropyridine is used as a raw material to be reacted with a chlorination reagent at set temperature under the action of a strong base and an additive to obtain the 4-tert-butyl-2,6-dichloro-pyridine. The route of the invention has the advantages of shortreaction steps, mild conditions and simple operation and is suitable for large-scale preparation of the 4-tert-butyl-2-chloropyridine and the 4-tert-butyl-2,6-dichloro-pyridine.
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Paragraph 0017; 0019
(2019/08/06)
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- ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT USING THE SAME
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PROBLEM TO BE SOLVED: To provide a compound which has an electron-donating property and is stable in the atmosphere. SOLUTION: The organic compound is represented by general formula [1] (where n represents an integer from 0 to 3 inclusive; R1 and R4 each represent an alkyl group or an aryl group selected from a phenyl group, a naphthyl group, a biphenyl group, a terphenyl group, a phenanthrenyl group, a fluorenyl group, and a fluoranthenyl group; when R1 or R4 is an aryl group, the aryl group may further have an alkyl group; R2 and R3 each represent an alkyl group or an aryl group selected from a phenyl group, a naphthyl group, a biphenyl group, a terphenyl group, a phenanthryl group, a fluorenyl group, and a fluoranthenyl group; when R2 or R3 is an aryl group, the aryl group may further have an alkyl group, a phenyl group, or a naphthyl group; when R1 and R4 are alkyl groups, R2 and R3 are aryl groups; and when R2 and R3 are alkyl groups, R1 and R4 are aryl groups). SELECTED DRAWING: None COPYRIGHT: (C)2017,JPO&INPIT
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- Stereo- and Regioselective Alkyne Hydrometallation with Gold(III) Hydrides
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The hydroauration of internal and terminal alkynes by gold(III) hydride complexes [(C^N^C)AuH] was found to be mediated by radicals and proceeds by an unexpected binuclear outer-sphere mechanism to cleanly form trans-insertion products. Radical precursors such as azobisisobutyronitrile lead to a drastic rate enhancement. DFT calculations support the proposed radical mechanism, with very low activation barriers, and rule out mononuclear mechanistic alternatives. These alkyne hydroaurations are highly regio- and stereospecific for the formation of Z-vinyl isomers, with Z/E ratios of >99:1 in most cases.
- Pintus, Anna,Rocchigiani, Luca,Fernandez-Cestau, Julio,Budzelaar, Peter H. M.,Bochmann, Manfred
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p. 12321 - 12324
(2016/10/13)
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- Heteroleptic Ir(III) phosphors with bis-tridentate chelating architecture for high efficiency OLEDs
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A bis-tridentate iridium complex represented by a formula (I): where R3 to R8, R21 to R23, R9, R10, X1, X2, and X3 are as defined in the specification.
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- 2-Amino-1,3,5-triazine chemistry: hydrogen-bond networks, Takemoto thiourea catalyst analogs, and olfactory mapping of a sweet-smelling triazine
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Abstract The chemistry of 4,6-dialkyl-2-amino-1,3,5-triazines with bulky alkyl substituents was investigated and their use as building blocks for preparing chiral thiourea organocatalysts explored. Reaction of ammonia with 4,6-di-tert-butyl-2-chloro-1,3,5-triazine gave 4,6-di-tert-butyl-1,3,5-triazin-2-amine which formed extended hydrogen-bond networks in the solid state according to X-ray crystallography. Selected heterocyclic amines were converted to isothiocyanates, and the latter reacted with (S,S)-2-(dimethylamino)cyclohexylamine to give enantiopure 1-hetaryl-3-[2-(dimethylamino)cyclohexyl]thioureas, with hetaryl representing either 4,6-dimethyl-1,3-diazin-2-yl, 4,6-diisopropyl-1,3,5-triazin-2-yl, or 4,6-di-tert-butyl-1,3,5-triazin-2-yl groups. These compounds are structural analogs of Takemotos's chiral thiourea organocatalysts (1-[3,5-bis(trifluoromethyl)phenyl]-3-[(1S,2S)-2-(dimethylamino)cyclohexyl]thiourea) with an aza-aryl instead of the 3,5-bis(trifluoromethyl)phenyl group. They feature a strong intramolecular N-H to N-1 hydrogen bond, as shown by X-ray crystallography of 1-(4,6-di-tert-butyl-1,3,5-triazin-2-yl)-3-[2-(dimethylamino)cyclohexyl]thiourea in the solid state and by 1H NMR spectroscopy of all derivatives in CDCl3 solution, which prevents them from acting as bifunctional organocatalyst. In the reaction of 4,6-di-tert-butyl-2-chloro-1,3,5-triazine with ammonia, 4,6-di-tert-butyl-2-ethoxy-1,3,5-triazine was identified as side-product displaying a mildly sweet, floral odor that is unusual for a 1,3,5-triazine. Analogs (>35) of 4,6-di-tert-butyl-2-ethoxy-1,3,5-triazine were prepared to define the important structural factors of the olfactophore.
- Hintermann, Lukas,P?thig, Alexander,Xiao, Li
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p. 1529 - 1539
(2015/08/18)
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- Substituted 2,2′-bipyridines by nickel catalysis: 4,4′-Di- tert -butyl-2,2′-bipyridine
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A simple, ligand-free synthesis of the important bipyridyl ligand 4,4′-di-tert-butyl-2,2′-bipyridine is presented. 5,5′-Bis(trifluoromethyl)-2,2′-bipyridine is also synthesized by the same protocol. The syntheses efficiently couple the parent 2-chloropyridines by a nickel-catalyzed dimerization with manganese powder as the terminal reductant. Georg Thieme Verlag Stuttgart New York.
- Buonomo, Joseph A.,Everson, Daniel A.,Weix, Daniel J.
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p. 3099 - 3102
(2013/12/04)
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- PYRIDINE AND ISOQUINOLINE DERIVATIVES AS SYK- AND JAK-KINASE INHIBITORS
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The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.
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- Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
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The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.
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- Charged cyclometalated iridium(III) complexes that have large electrochemical gap
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Bis-cyclometalated cationic Ir(III) diimine complexes [Ir(C^N) 2(N^N)](PF6) with 1-phenylpyrazoles (C^N) and 1-(4′-tert-butyl-2′-pyridyl)pyrazole (N^N) are white solids that have absorption onset below 425 nm and electrochemical gap of up to 3.5 V.
- Shavaleev, Nail M.,Scopelliti, Rosario,Baranoff, Etienne,Graetzel, Michael,Nazeeruddin, Mohammad K.
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scheme or table
p. 316 - 319
(2012/04/23)
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- Bright blue phosphorescence from cationic bis-cyclometalated iridium(III) isocyanide complexes
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We report new bis-cyclometalated cationic iridium(III) complexes [(CN) 2Ir(CN-tert-Bu)2](CF3SO3) that have tert-butyl isocyanides as neutral auxiliary ligands and 2-phenylpyridine or 2-(4'- fluorophenyl)-R-pyridines (where R is 4-methoxy, 4-tert-butyl, or 5-trifluoromethyl) as CN ligands. The complexes are white or pale yellow solids that show irreversible reduction and oxidation processes and have a large electrochemical gap of 3.58-3.83 V. They emit blue or bluegreen phosphorescence in liquid/solid solutions from a cyclometalatingligand- centered excited state. Their emission spectra show vibronic structure with the highest-energy luminescence peak at 440-459 nm. The corresponding quantum yields and observed excitedstate lifetimes are up to 76% and 46 μs, respectively, and the calculated radiative lifetimes are in the range of 46-82 μs. In solution, the photophysical properties of the complexes are solvent-independent, and their emission color is tuned by variation of the substituents in the cyclometalating ligand. For most of the complexes, an emission color red shift occurs in going from solution to neat solids. However, the shift is minimal for the complexes with bulky tert-butyl or trifluoromethyl groups on the cyclometalating ligands that prevent aggregation. We report the first example of an iridium(III) isocyanide complex that emits blue phosphorescence not only in solution but also as a neat solid.
- Shavaleev, Nail M.,Monti, Filippo,Costa, Ruben D.,Scopelliti, Rosario,Bolink, Henk J.,Orti, Enrique,Accorsi, Gianluca,Armaroli, Nicola,Baranoff, Etienne,Graetzel, Michael,Nazeeruddin, Mohammad K.
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scheme or table
p. 2263 - 2271
(2012/05/20)
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- Intra- and intermolecular C-H activation by bis(phenolate) pyridineiridium(III) complexes
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A bis(phenolate)pyridine pincer ligand (henceforth abbreviated as ONO) has been employed to support a variety of iridium complexes in oxidation states I, III, and IV. Complexes (ONO)IrL2Me (L = PPh3, PEt 3) react with I2 to cleave the Ir-C bond and liberate MeI, apparently via a mechanism beginning with electron transfer to generate an intermediate Ir(IV) complex, which can be isolated and characterized for the case L = PEt3. The PPh3 complex is transformed in benzene at 65 °C to the corresponding phenyl complex, with loss of methane, and subsequently to a species resulting from metalation of a PPh3 ligand. Labeling and kinetics studies indicate that PPh3 is the initial site of C-H activation, even though the first observed product is that resulting from intermolecular benzene activation. C-H activation of acetonitrile has also been observed.
- Fu, Ross,Bercaw, John E.,Labinger, Jay A.
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experimental part
p. 6751 - 6765
(2012/02/05)
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- Alkylation of Pyridine in Free Radical Chain Reactions Utilizing Alkylmercurials
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Pyridines or N,N,N',N'-tetramethyl-p-phenylenediamine will undergo a photostimulated free radical chain reaction with alkylmercury halides or carboxylates, yielding ring alkylated substitution products.Alkene mercuration products (R1CH(Y)CH(R2)HgX with Y=HO, RO, CH3CONH; X=Cl, CH3CO2, CF3CO2) can be used without isolation for the alkylation reaction
- Russell, Glen A.,Guo, Deliang,Khanna, Rajive K.
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p. 3423 - 3425
(2007/10/02)
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