- Compound with AMPK agonistic activity and preparation and application of prodrug thereof
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The invention relates to a compound with AMPK agonistic activity and a prodrug thereof, and as well as a preparation method and medical application of a prodrug thereof. The compound has the structure shown in the formula (I), and the prodrug of the compound has the structure shown in the formula (II), wherein each group and the substituent are as defined in the specification. The invention discloses a preparation method of the compound and application of the compound in prevention and treatment AMPK related diseases, and the AMPK related diseases include, but are not limited to, energy metabolism abnormality related diseases. Neurodegenerative diseases and inflammation-related diseases and the like.
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Paragraph 0145; 0149-0150; 0239; 0243-0244
(2021/10/27)
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- Transformations of Aryl Ketones via Ligand-Promoted C?C Bond Activation
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The coupling of aromatic electrophiles (aryl halides, aryl ethers, aryl acids, aryl nitriles etc.) with nucleophiles is a core methodology for the synthesis of aryl compounds. Transformations of aryl ketones in an analogous manner via carbon–carbon bond activation could greatly expand the toolbox for the synthesis of aryl compounds due to the abundance of aryl ketones. An exploratory study of this approach is typically based on carbon–carbon cleavage triggered by ring-strain release and chelation assistance, and the products are also limited to a specific structural motif. Here we report a ligand-promoted β-carbon elimination strategy to activate the carbon–carbon bonds, which results in a range of transformations of aryl ketones, leading to useful aryl borates, and also to biaryls, aryl nitriles, and aryl alkenes. The use of a pyridine-oxazoline ligand is crucial for this catalytic transformation. A gram-scale borylation reaction of an aryl ketone via a simple one-pot operation is reported. The potential utility of this strategy is also demonstrated by the late-stage diversification of drug molecules probenecid, adapalene, and desoxyestrone, the fragrance tonalid as well as the natural product apocynin.
- Dai, Hui-Xiong,Li, Hanyuan,Li, Ling-Jun,Liu, Qi-Sheng,Ma, Biao,Wang, Mei-Ling,Wang, Xing,Wang, Zhen-Yu,Xu, Hui
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p. 14388 - 14393
(2020/07/06)
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- Phenylpyridine derivative (by machine translation)
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[Problem] in a photoelectric conversion element, the heat resistance can be improved phenylpyridine derivative. (1) Represented by the formula [a] phenylpyridine derivative (A ring, B, C D and is, a pyridine ring, each of the carbon atoms contained in R1 - R11, hydrogen, straight-chain alkyl group, a branched alkyl group, an aryl group, such as one selected from binding. ). Figure 1 [drawing] (by machine translation)
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Paragraph 0040
(2020/02/01)
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- Palladium-Catalyzed Decarbonylative Borylation of Carboxylic Acids: Tuning Reaction Selectivity by Computation
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Decarbonylative borylation of carboxylic acids is reported. Carbon electrophiles are generated directly after reagent-enabled decarbonylation of the in situ accessible sterically-hindered acyl derivative of a carboxylic acid under catalyst controlled conditions. The scope and the potential impact of this method are demonstrated in the selective borylation of a variety of aromatics (>50 examples). This strategy was used in the late-stage derivatization of pharmaceuticals and natural products. Computations reveal the mechanistic details of the unprecedented C?O bond activation of carboxylic acids. By circumventing the challenging decarboxylation, this strategy provides a general synthetic platform to access arylpalladium species for a wide array of bond formations from abundant carboxylic acids. The study shows a powerful combination of experiment and computation to predict decarbonylation selectivity.
- Liu, Chengwei,Ji, Chong-Lei,Hong, Xin,Szostak, Michal
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supporting information
p. 16721 - 16726
(2018/11/30)
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- Triaryl boron derivatives of pyridine as electron transporting materials for blue phosphorescent organic light-emitting diodes
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Two duryl borane derivatives, tris(2,3,5,6-tetramethyl-4-(pyridin-3-yl)phenyl)borane (TDPB) and tris(2,3,5,6-tetramethyl-4'-(pyridin-3-yl)biphenyl-4-yl)borane (TDPPB), which contain heteroaromatic pyridine rings at peripheral positions were synthesized to
- Lee, Jiewon,Lee, Sunhee,Kim, Jin-Hyoung,Kang, Sang Ook,Han, Won-Sik
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- Transition-Metal-Free, Visible-Light-Enabled Decarboxylative Borylation of Aryl N-Hydroxyphthalimide Esters
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Herein, we report a conceptually novel borylation reaction proceeding via a mild photoinduced decarboxylation of redox-activated aromatic carboxylic acids. This work constitutes the first application of cheap and easily prepared N-hydroxyphthalimide esters as aryl radical precursors and does not require the use of expensive transition metals or ligands. The reaction is operationally simple, scalable, and displays broad scope and functional group tolerance.
- Candish, Lisa,Teders, Michael,Glorius, Frank
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p. 7440 - 7443
(2017/06/13)
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- Octahedral [Pd6L8]12+ Metallosupramolecular Cages: Synthesis, Structures and Guest-Encapsulation Studies
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Four planar tripyridyl ligands (Ltripy), 1,3,5-tris(pyridin-3-ylethynyl)benzene 1 a, 1,3,5-tris[4-(3-pyridyl)phenyl]benzene 2 a, and the hexyloxy chain functionalized derivatives 1,3,5-tris[(3-hexyloxy-5-pyridyl)ethynyl]benzene 1 b, and 1,3,5-tris[4-(3-hexyloxy-5-pyridyl)phenyl]benzene 2 b, were synthesized and used to generate a family of [Pd6(Ltripy)8](BF4)12 octahedral cages (Ltripy=1 a, b or 2 a, b). The ligands and cages were characterized using a combination of 1H, 13C, and DOSY nuclear magnetic resonance (NMR) spectroscopy, high resolution electrospray mass spectrometry (HR-ESI-MS), infrared (IR) spectroscopy, elemental analysis, and in three cases, X-ray crystallography. The molecular recognition properties of the cages with neutral and anionic guests were examined, in dimethyl sulfoxide (DMSO), using NMR spectroscopy, mass spectrometry and molecular modeling. No binding was observed with simple aliphatic and aromatic guest molecules. However, anionic sulfonates were found to interact with the octahedral cages and the binding interaction was size selective. The smaller [Pd6(1 a, b)8]12+ cages were able to interact with three p-toluenesulfonate guest molecules while the larger [Pd6(2 a, b)8]12+ systems could host four of the anionic guest molecules. To probe the importance of the hydrophobic effect, a mixed water–DMSO (1:1) solvent system was used to reexamine the binding of the neutral organic guests adamantane, anthracene, pyrene and 1,8-naphthalimide within the cages. In this solvent system all the guests except adamantane were observed to bind within the cavities of the cages. NMR spectroscopy and molecular modeling indicated that the cages bind multiple copies of the individual guests (between 3–6 guest molecules per cage).
- Kim, Tae Y.,Digal, Lori,Gardiner, Michael G.,Lucas, Nigel T.,Crowley, James D.
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p. 15089 - 15097
(2017/10/11)
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- Compound containing quinoxaline and pyridine groups and organic electroluminescent device thereof
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The invention provides an organic electroluminescent compound containing quinoxaline and pyridine groups. The compound has better heat stability, high luminous efficiency and high luminous purity, can be used for manufacturing an organic electroluminescent device, and is applied to the field of organic solar cells, organic thin film transistors or organic photoreceptors. The invention also provides the organic electroluminescent device, which comprises an anode, a cathode and an organic layer, wherein the organic layer includes more than one layer in a luminous layer, a hole injection layer, a hole transporting layer, a hole blocking layer, and electron injection layer and an electron transporting layer; at least one layer in the organic layer contains a compound as shown by a structural formula I which is as shown in the description.
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- An electron transport material and an organic electroluminescence element using the same
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The compound represented by formula (1) is characterized in being stable in a thin film state even when voltage is applied, and in having a high charge- transporting capability. This compound is suitable for a charge transport material for an organic EL element, and by using this electron transport material in the electron transport layer and/or electron injection layer of an organic EL element, an organic EL element having a long life can be obtained. In formula (1), Py is pyridyl, any hydrogen of this pyridyl can be substituted by an alkyl, cycloalkyl, phenyl, 1-naphthyl, or 2-naphthyl, and the phenyl, 1-naphthyl, or 2-naphthyl can be further substituted by an alkyl or cycloalkyl; R is hydrogen, an alkyl, a cycloalkyl, or an aryl, and any hydrogen of this aryl can be substituted by an alkyl or cycloalkyl.
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Paragraph 0186
(2016/10/08)
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- NOVEL COMPOUND, ORGANIC ELECTROLUMINESCENT ELEMENT, ILLUMINATION DEVICE AND DISPLAY DEVICE
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PROBLEM TO BE SOLVED: To provide novel long-life compounds, organic electroluminescent elements, illumination devices and display devices. SOLUTION: This invention relates to a compound represented by formula (1) (where rings A, B, C, and D are pyridine rings; R1-11 are H, an alkyl group, an aryl group or the like). COPYRIGHT: (C)2016,JPO&INPIT
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Paragraph 0034; 0037-0040
(2016/10/08)
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- Synthesis of trimethylstannyl arylboronate compounds by sandmeyer-type transformations and their applications in chemoselective cross-coupling reactions
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A synthetic method based on Sandmeyer-type reactions to access both tin- and boron-substituted arenes from nitroaniline derivatives is described. This transformation can be applied to the synthesis of a series of functionalized trimethylstannyl arylboronates. In addition, the chemoselective reaction of the Stille and Suzuki-Miyaura cross-coupling reactions is explored, and a series of m- and p-terphenyl derivatives have been synthesized by conducting consecutive one-pot Stille and Suzuki-Miyaura cross-coupling reactions.
- Qiu, Di,Wang, Shuai,Tang, Shengbo,Meng, He,Jin, Liang,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
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p. 1979 - 1988
(2014/04/03)
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- Synthesis of aryl trimethylstannanes from aryl amines: A sandmeyer-type stannylation reaction
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Sandmeyer-type stannylation: Stille coupling is one of the most powerful coupling reactions for C-C bond formation, whereas there are only limited methods to access aryl stannane compounds. A mild stannylation process based on a Sandmeyer-type transformation using aromatic amines as the starting materials is described. DCE: 1,2-dichloroethane. Copyright
- Qiu, Di,Meng, He,Jin, Liang,Wang, Shuai,Tang, Shengbo,Wang, Xi,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
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p. 11581 - 11584
(2013/11/06)
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- Novel four-pyridylbenzene-armed biphenyls as electron-transport materials for phosphorescent OLEDs
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A series of four-pyridylbenzene-armed biphenyl derivatives were designed and synthesized as an electron-transport and exciton- and hole-block layer for the fac-tris(2-phenylpyridine)iridium (lr(PPy)3)-based green phosphorescent organic light-em
- Su, Shi-Jian,Tanaka, Daisaku,Li, Yan-Jun,Sasabe, Hisahiro,Takeda, Takashi,Kido, Junji
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supporting information; experimental part
p. 941 - 944
(2009/04/07)
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