- Highly efficient heterogeneous V2O5@TiO2 catalyzed the rapid transformation of boronic acids to phenols
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A V2O5@TiO2 catalyzed green and efficient protocol for the hydroxylation of boronic acid into phenol has been developed utilizing environmentally benign oxidant hydrogen peroxide. A wide range of electron-donating and the electron-withdrawing group-containing (hetero)aryl boronic acids were transformed into their corresponding phenol. The methodology was also applied successfully to transform various natural and bioactive molecules like tocopherol, amino acids, cinchonidine, vasicinone, menthol, and pharmaceuticals such as ciprofloxacin, ibuprofen, and paracetamol. The other feature of the methodology includes gram-scale synthetic applicability, recyclability, and short reaction time.
- Upadhyay, Rahul,Singh, Deepak,Maurya, Sushil K.
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supporting information
p. 3925 - 3931
(2021/08/24)
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- 4-((6-(2-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-2-OXOETHYL) PYRIDIN-3-YL)OXY)BENZONITRILE AND PROCESSES OF PREPARATION
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Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-2-oxoethyl)pyridin-3-yl)oxy)benzonitrile.
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Page/Page column 4; 5
(2017/06/12)
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- 4-((6-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-2-HYDROXY-3-(1H-1,2,4-TRIAZOL-1-YL)PROPYL)PYRIDIN-3-YL)OXY)BENZONITRILE AND PROCESSES OF PREPARATION
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Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1,1- difluoro-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
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Page/Page column 5; 6
(2017/06/12)
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- 4-((6-2-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-2-HYDROXY-3-(1H-1,2,4-TRIAZOL-1-YL)PROPYL)PYRIDIN-3-YL)OXY)BENZONITRILE AND PROCESSES OF PREPARATION
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Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1, 1- difluoro-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
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Page/Page column 5; 6
(2017/06/12)
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- Synthesis of 9,9′-Spirobifluorenes and 4,5-Diaza-9,9′-spirobifluorenes and Their Application as Affinity Materials for Quartz Crystal Microbalances
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Two different classes of aza analogues of 9,9′-spirobifluorenes have been synthesized. These were obtained by either furnishing the spirobifluorene with additional pyridyl moieties or by installing the aza function directly into the spirobifluorene core. These structurally rigid compounds were then evaluated as affinity materials for quartz crystal microbalances and proved to be highly potent for the detection of volatile organic compounds.
- Stobe, Caroline,Pyka, Isabella,Linke, Alexander,Müller, Sarah,Schnakenburg, Gregor,Waldvogel, Siegfried R.,Lützen, Arne
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p. 758 - 769
(2017/06/06)
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- HEDGEHOG ANTAGONISTS HAVING ZINC BINDING MOIETIES
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The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The com-pounds can be used in methods of treating proliferative dis-eases and disorders such as cancer
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Paragraph 0162; 0183
(2014/02/16)
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- Synthesis of pyridine-N-oxide-borane intramolecular complexes by palladium-catalyzed reaction of 2-bromopyridine-N-oxides with alkynyltriarylborates
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Pyridine-N-oxide-borane intramolecular complexes having an aza-stilbene π-framework were synthesized by the palladium-catalyzed reaction of 2-bromopyridine-N-oxides with alkynyltriarylborates.
- Ishida, Naoki,Ikemoto, Wataru,Narumi, Mizuna,Murakami, Masahiro
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supporting information; experimental part
p. 3008 - 3011
(2011/08/05)
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- Catalytic chain-breaking pyridinol antioxidants
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(Chemical Equation Presented) The synthesis of 3-pyridinols carrying alkyltelluro, alkylseleno, and alkylthio groups is described together with a detailed kinetic, thermodynamic, and mechanistic study of their antioxidant activity. When assayed for their capacity to inhibit azo-initiated peroxidation of linoleic acid in a water/chlorobenzene two-phase system, tellurium-containing 3-pyridinols were readily regenerable by N-acetylcysteine contained in the aqueous phase. The best inhibitors quenched peroxyl radicals more efficiently than α-tocopherol, and the duration of inhibition was limited only by the availability of the thiol reducing agent. In homogeneous phase, inhibition of styrene autoxidation absolute rate constants kinh for quenching of peroxyl radical were as large as 1 x 107 M-1 s -1, thus outperforming the best phenolic antioxidants including α-tocopherol. Tellurium-containing 3-pyridinols could be quantitatively regenerated in homogeneous phase by N-tert-butoxycarbonyl cysteine methyl ester, a lipid-soluble analogue of N-acetylcysteine. In the presence of an excess of the thiol, a catalytic mode of action was observed, similar to the one in the two-phase system. Overall, compounds bearing the alkyltelluro moiety ortho to the OH group were much more effective antioxidants than the corresponding para isomers. The origin of the high reactivity of these compounds was explored using pulse-radiolysis thermodynamic measurements, and a mechanism for their unusual antioxidant activity was proposed. The tellurium-containing 3-pyridinols were also found to catalyze reduction of hydrogen peroxide in the presence of thiol reducing agents, thereby acting as multifunctional (preventive and chain-breaking) catalytic antioxidants.
- Kumar, Sangit,Johansson, Henrik,Kanda, Takahiro,Engman, Lars,Mueller, Thomas,Bergenudd, Helena,Jonsson, Mats,Pedulli, Gian Franco,Amorati, Riccardo,Valgimigli, Luca
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supporting information; experimental part
p. 716 - 725
(2010/06/13)
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- COMPOUNDS COMPRISING A 3-PYRIDINOL OR 5-PYRIMIDINOL RING HAVING AN ORGANOSELENO OR ORGANOTELLURO SUBSTITUENT FOR USE AS ANTIOXIDANTS
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Compounds comprising a 3-pyridinol or 5-pyrimidinol ring carrying an organoseleno- or organotelluro- substituent on the pyridine or pyrimidine ring, exhibit useful antioxidant properties. The compounds may for example be in accordance with the following formula (I) as defined herein. Catalytic chain-breaking and hydroperoxide decomposing antioxidant properties are also disclosed. Furthermore the compounds may be used in combination with a reducing agent. The compounds are useful for the stabilization of man-made and natural materials, or for the prevention or treatment of disorders caused by or involving free radical-mediated or oxidative tissue damage.
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Page/Page column 39
(2009/12/27)
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- Catalytic chain-breaking pyridinol antioxidants
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(Chemical Equation Presented) When assayed for their capacity to inhibit azo-initiated peroxidation of linoleic acid in a water/chlorobenzene two-phase system, tellurium-containing 3-pyridinols were readily regenerable by N-acetylcysteine contained in the aqueous phase. The best inhibitors quenched peroxyl radicals more efficiently than α-tocopherol, and the duration of inhibition was limited only by the availability of the thiol reducing agent. The compounds were also found to catalyze reduction of hydrogen peroxide in the presence of thiol reducing agent.
- Kumar, Sangit,Johansson, Henrik,Kanda, Takahiro,Engman, Lars,Mueller, Thomas,Jonsson, Mats,Pedulli, Gian Franco,Petrucci, Silvia,Valgimigli, Luca
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supporting information; experimental part
p. 4895 - 4898
(2009/05/31)
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- HETEROCYCLE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVE
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Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): (wherein X1 to X4 represent a carbon atom, etc., ring A represents a 5- or 6-membered heteroaryl having from 1 to 4 hetero atoms selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom, X5 represent an oxygen atom, etc., X represent a carbon atom, etc., Het represents a 5- or 6-membered aliphatic hetero ring, R1 represents aryl, etc., R2 represents formyl, etc., R3 represents -C1-6 alkyl, etc.), as well as their pharmaceutically acceptable salts.
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Page/Page column 58
(2010/11/30)
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- SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR
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Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
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Page/Page column 90
(2015/10/07)
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- Efficient synthesis of halohydroxypyridines by hydroxydeboronation
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This paper describes a general method for the synthesis of halohydroxypyridines from novel halopyridinylboronic acids and esters recently described by some of us. Halopyridinylboronic acids and esters have been efficiently hydroxydeboronated under mild conditions by employing hydrogen peroxide or meta-chloroperbenzoic acid. These hydroxylations take place regioselectively without other oxidation (N-oxide formation).
- Voisin, Anne Sophie,Bouillon, Alexandre,Lancelot, Jean-Charles,Rault, Sylvain
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p. 1417 - 1421
(2007/10/03)
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- Ring nitrogen-substituted non-steroidal estrogens: Pyridine and pyrimidine analogs of the phenol in deoxyhexestrol experience resonance constraints on preferred ligand conformation
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Pyridine and pyrimidine analogs of the non-steroidal estrogen deoxyhexestrol were synthesized. Their low affinity for the estrogen receptor is ascribed, in part, to resonance enforcement of a conformation unfavorable for binding. To develop compounds selective for estrogen receptor beta (ERβ), we substituted hydroxypyridine and pyrimidine heteroaryl groups for the characteristic phenol ring of non-steroidal estrogens. The unexpectedly low affinity showed by some of these compounds is ascribed, in part, to a resonance-enforced conformational constraint that prevents their optimal accommodation in the ER ligand binding pocket.
- De Angelis, Meri,Katzenellenbogen, John A.
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p. 5835 - 5839
(2007/10/03)
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- 3-Pyridyl enantiomers and their use as analgesics
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The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: STR1 or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.
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- Furopyridine, thienopyridine pyrrolopyridine useful in controlling chemical synaptic transmission
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Novel heterocyclic ether compounds having the formula: STR1 wherein A, m, R, X, Y1, Y2 and Y3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.
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