- The organic electroluminescent element material and using the material of the organic electroluminescent element
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Provided are: an organic electroluminescent element (organic EL element) having improved element light emission efficiency, ensuring sufficient drive stability, and having a simple configuration; and a material for organic EL elements, used in same. This
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Paragraph 0093; 0094
(2018/04/14)
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- Design and synthesis of nonsteroidal progesterone receptor antagonists based on C,C′-diphenylcarborane scaffold as a hydrophobic pharmacophore
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The progesterone receptor (PR) plays important roles in multiple physiological processes, including female reproduction. Here, we report the synthesis of nonsteroidal PR antagonists containing a boron cluster as the hydrophobic core. We found that 1,7-diphenyl-meta-carborane was the preferred substructure among the three carborane isomers. Compound 39 was the most potent PR antagonist (IC50: 29 nM). Compound 41 also exhibited potent activity (IC50: 93 nM), and did not bind to androgen receptor, glucocorticoid receptor or mineralocorticoid receptor. These compounds may be useful for investigating potential clinical applications of PR modulators.
- Fujii, Shinya,Yamada, Ayumi,Nakano, Eiichi,Takeuchi, Yuki,Mori, Shuichi,Masuno, Hiroyuki,Kagechika, Hiroyuki
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p. 264 - 277
(2014/08/05)
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- Lipase-catalyzed asymmetric acylation of boron cluster-containing secondary alcohols
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The lipase-catalyzed asymmetric acetylation of secondary alcohols containing a carborane (boron cluster) moiety was investigated. Most lipases examined showed poor catalytic activity toward carborane-containing secondary alcohol 1a, but lipase TL efficiently catalyzed the acetylation of 1a with high enantioselectivity, to afford (R)-3a. This selectivity is similar to that of the general lipase-catalyzed acylation of secondary alcohols. Utilizing lipase TL, we succeeded in the resolution of carborane-containing alcohol 5, synthesized as a progesterone receptor ligand candidate, and evaluated the activities of the two enantiomers.
- Mori, Shuichi,Takagaki, Ryohei,Fujii, Shinya,Matsumura, Mio,Tanatani, Aya,Kagechika, Hiroyuki
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p. 1505 - 1512
(2015/01/16)
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- C-arylation and C-heteroarylation of icosahedral carboranes via their copper(I) derivatives
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Reaction between C-mono- or C,C'-di-copper(I) derivatives of 1,2- 1,7-, or 1,12-dicarba-closo-dodecaborane(12) and aryl iodides in the presence of pyridine gives the corresponding C-mono- or C,C'-diaryl derivatives of 1,7- and 1,12-dicarba-closo-dodecaboranes(12); 1,2-dicarba-closo-dodecaborane(12) gives only the C-monoaryl product.Cyclic or linear arylene coupled systems are obtained when di-iodoarenes are used.Copper(I) derivatives may be generated from C-unsubstituted or C-monosubstituted carboranes using copper(I) t-butoxide when substituents incompatible with the use of C-lithio-intermediates are involved.The C-copper(I) derivative of 1,2-dicarba-closo-dodecaborane(12) gives 1,2-di-2'-pyridyl-1,2-dicarba-closo-dodecaborane(12) specifically with 2-bromopyridine.The (inferred) intermediate mono-2-pyridyl-derivative, obtained independently from 2-ethynylpyridine and the dimethylsulphide complex of decaborane, gives 1-phenyl-2,2'-pyridyl-1,2-dicarba-closo-dodecaborane(12) upon conversion into its copper(I) derivative and treatment with iododobenzene.However, the copper(I) derivative of 1-phenyl-1,2-dicarba-closo-dodecaborane(12) does not react to a significant extent with 2-bromopyridine.
- Coult, Robert,Fox, Mark A.,Gill, Wendy R.,Herbertson, Penelope L.,MacBride, J.A. Hugh,Wade, Kenneth
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- Carborane reductive-elimination reaction from a six-coordinate hydridocarboranyliridium(III) complex: Kinetic and mechanistic study
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A kinetic and mechanistic study of the reductive-elimination reaction of the carborane 1-H-T-C6H5-1,7-C2B10H10 (H-carb) from the six-coordinate iridium(III) complex Ir(H)(Cl)(σ-carb)(CO)(PPh3)2 has been carried out in 1,2-dichloroethane by IR spectroscopy between 20 and 50°C. The mechanism of the carborane-elimination reaction implies a preliminary PPh3 dissociation to give the five-coordinate Ir(H)(Cl)(σ-carb)(CO)(PPh3) complex. This intermediate then undergoes a reductive elimination of the carborane molecule through two pathways: (i) direct elimination to give the three-coordinate iridium(I) complex, IrCl(CO)(PPh3); (ii) a phosphine-induced elimination via trans → cis isomerization of the H and carb ligands. The kinetic and thermodynamic parameters are also reported and discussed.
- Basato,Morandini,Longato,Bresadola
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p. 649 - 653
(2008/10/08)
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