- A FACILE SYNTHESIS OF BROMO-2-ALKOXYPYRIDINES
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Several bromo-2-methoxypyridines 2a-2e and bromo-2-benzyloxypyridines 2a'-2e' were synthesised by the reaction of bromo-substituted 2-pyridones 1 which were reacted with alkyl halides in the presence of silver carbonate in benzene.
- Shiao, Min-Jen,Tarng, Kai-Yih
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- AMIDE COMPOUND AND PHARMACEUTICAL COMPRISING SAME
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Provided is a novel compound which has an excellent Aβ aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH2—, —O—, —S—, or —NH—; R1 and R2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group.
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Paragraph 0087-0089
(2016/10/31)
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- Mild and Regioselective N-Alkylation of 2-Pyridones in Water
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A mild and regioselective N-alkylation reaction of 2-pyridones in water has been developed. Tween 20 (2% w/w) was added to create a micellar system for improved solubility of starting materials, which leads to enhanced reaction rates. The protocol demonstrated a wide substrate scope with good isolated yields (40-94%) for all of the 24 examples evaluated. High regioselectivity favoring N-alkylation over O-alkylation was observed for benzyl halides (>5:1), primary alkyl halides (>6:1), and bulky and less reactive secondary alkyl halides (>2.4:1).
- Hao, Xin,Xu, Zhongmiao,Lu, Hongfu,Dai, Xuedong,Yang, Ting,Lin, Xichen,Ren, Feng
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supporting information
p. 3382 - 3385
(2015/07/28)
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- Synthesis of mono- and diaza-'pyridones' via stille coupling of alkoxystannanes
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Various alkoxy-substituted heterocyclic stannanes provide access to the corresponding substituted 'pyridone' moieties via Stille cross-coupling. Both pyridyl and a series of diazinyl stannanes are prepared, and options for unmasking (via demethylation or debenzylation) of the pyridone unit are evaluated. Georg Thieme Verlag Stuttgart. New York.
- Smith, Charlotte L.,Hirschh?user, Christoph,Malcolm, Georgia K.,Nasrallah, Daniel J.,Gallagher, Timothy
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p. 1904 - 1908
(2014/08/18)
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- Discovery and biological profiling of potent and selective mTOR inhibitor GDC-0349
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Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer. Optimization of advanced lead 1 culminated in the discovery of clinical development candidate 8h, GDC-0349, a potent and selective ATP-competitive inhibitor of mTOR. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.
- Pei, Zhonghua,Blackwood, Elizabeth,Liu, Lichuan,Malek, Shiva,Belvin, Marcia,Koehler, Michael F. T.,Ortwine, Daniel F.,Chen, Huifen,Cohen, Frederick,Kenny, Jane R.,Bergeron, Philippe,Lau, Kevin,Ly, Cuong,Zhao, Xianrui,Estrada, Anthony A.,Truong, Tom,Epler, Jennifer A.,Nonomiya, Jim,Trinh, Lan,Sideris, Steve,Lesnick, John,Bao, Linda,Vijapurkar, Ulka,Mukadam, Sophie,Tay, Suzanne,Deshmukh, Gauri,Chen, Yung-Hsiang,Ding, Xiao,Friedman, Lori S.,Lyssikatos, Joseph P.
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supporting information
p. 103 - 107
(2013/02/26)
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- TRIAZOLE DERIVATIVES HAVING ANTIFUNGAL ACTIVITY, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.
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Page/Page column 46-47
(2009/01/24)
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- Microwave-promoted synthesis of amino-substituted 2-pyridone derivatives via palladium-catalyzed amination reaction
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A rapid and efficient synthesis of amino-substituted 2-pyridones was demonstrated by palladium-catalyzed amination reaction under microwave irradiation. This high-speed synthesis provided a number of amino-substituted 2-pyridones from the corresponding bromo-2-benzyloxypyridines via palladium-catalyzed amination followed by hydrogenolysis of benzyl ether.
- Heo, Jung-Nyoung,Young, Seob Song,Bum, Tae Kim
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p. 4621 - 4625
(2007/10/03)
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- ARYLPYRIDINE COMPOUNDS
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The present invention relates to arylpyridine compounds and methods of using them.
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- Thiazoles and thiopyridines: Novel series of high affinity h5HT 7 ligands
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A series of thiazole based 5HT7 ligands has been identified from screening. Optimisation of the pendent aryl group and modification of the core gave a related series of high affinity, selective thiopyridine based 5HT7 ligands, the most active of which behaves as a partial agonist.
- Thomson, Christopher G.,Beer, Margaret S.,Curtis, Neil R.,Diggle, Helen J.,Handford, Emma,Kulagowski, Janusz J.
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p. 677 - 680
(2007/10/03)
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- Exploiting the versatile assembly of arylpyridine fluorophores for wavelength tuning and SAR
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(Matrix presented) The facile modular assembly of polyarylpyridine fluorophores provides two important advantages in the development of fluorescent chemosensors: it allows rapid dissection of the structural requirements for fluorescent chemosensing and it allows dramatic tuning of emission wavelength by changes in a substituent remote from the binding site.
- Fang, Albert G.,Mello, Jesse V.,Finney, Nathaniel S.
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p. 967 - 970
(2007/10/03)
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- Method for treating neoplasia with amino or pyridylamino cyclobutene derivatives
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A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to amino or pyridylamino cyclobutane derivatives.
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- Herbicidal heterocyclic-substituted pyridines
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The present invention relates to 2,6-substituted pyridines of formula I, their preparation and use as herbicides.
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- Pentanuclear copper(II) complexes with the novel 6-(phenylethynyl)-2-pyridonate ligand: Synthesis, structures and magnetic properties
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Three pentanuclear copper(II) complexes, [Cu5(OMe)2(CF3CO2)(pehp) 6(Cl)] 1, [Cu5(OMe)2(CF3CO2)(pehp) 6-(NO3)] 2 and [Cu5(OH)(CF3CO2)3(pehp)6] 3, have been prepared via the solid-state reaction of hydrated copper(II) nitrate with the sodium salt of the novel ligand, 6-(phenylethynyl)-2-pyridone (Hpehp) in the presence of sodium trifluoroacetate. Crystal structural analysis at 220 K of 1-3 reveals capped-butterfly arrangements of the five copper atoms with the two shortest Cu ... Cu vectors in 1 and 2 [3.024(6)-3.050(3) A] occurring between the caps and the wingtips while in 3 the wingtip-cap distances are more asymmetric with one short [3.042(7) A] and one long [3.638(7) A] Cu ... Cu vector. Mass spectroscopic studies of 1-3 show fragmentation patterns consistent with the observed structures, while magnetic studies of the complexes indicate antiferromagnetic exchange coupling within the Cu5 cores and S = 1/2 ground states for all compounds. The trifluoroacetate adduct of Hpehp, Hpehp·0.5CF3CO2H was synthesised in three steps from 2-bromo-6-benzyloxypyridine via 2-benzyloxy-6-(phenylethynyl)pyridine and the single crystal X-ray structure of Hpehp was also determined.
- Doyle, Allan A.,Parsons, Simon,Solan, Gregory A.,Winpenny, Richard E. P.
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p. 2131 - 2137
(2007/10/03)
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- Acid-amide intermolecular hydrogen bonding
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A 2,2-dimethylbutynoic acid with a pyridone terminus (1) acts as its self-complement in molecular recognition to form an intermolecularly hydrogen-bonded dimer with hydrogen bonding between the amide and carboxylic acid group. The dimer is found in crystals of 1 by X-ray diffraction, in chloroform solution by 1H-NMR experiments and vapor pressure osmometry, and in the gas phase by FAB-MS.
- Wash, Paul L.,Maverick, Emily,Chiefari, John,Lightner, David A.
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p. 3802 - 3806
(2007/10/03)
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- Selective N-functionalization of 6-substituted-2-pyridones
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6-Substituted-2-pyridones can be selectively N-alkylated by treatment with NaH/LiBr in a mixture of DMF and DME. Yields of N-propargylated, N-allylated, and other N-functionalized products are good, and only small amounts of the isomeric O-alkylated produ
- Hui, Liu,Sung-Bo, Ko,Josien, Hubert,Curran, Dennis P.
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p. 8917 - 8920
(2007/10/02)
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- A CONVENIENT SYNTHESIS OF 2,4'-BIPYRIDINE
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2,4'-Bipyridine 6 was synthesized starting from N-ethoxycarbonylpyridinium chloride 1 and 2-benzyloxy-6-bromopyridine 2a or 6-bromo-2-methoxypyridine 2b via 6-benzyloxy-2,4'-bipyridine 3a or 6-methoxy-2,4'-bipyridine 3b and 6-chloro-2,4'-bipyridine 5.
- Shiao, Min-Jen,Tarng, Kai-Yih
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p. 637 - 641
(2007/10/02)
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