- SULFONAMIDES AS GPR40- AND GPR120-AGONISTS
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The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I). Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabet
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Page/Page column 22-23; 34
(2018/03/06)
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- Chain-Walking Polymerization of Linear Internal Octenes Catalyzed by α-Diimine Nickel Complexes
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The chain-walking polymerization of linear internal alkenes (i.e., trans-2-, 3-, and 4-octenes) using α-diimine nickel catalysts activated with modified methylaluminoxane (MMAO) was studied in comparison with the corresponding terminal alkene polymerization. The rates of polymerization were found to decrease in the following order: 1-octene > 4-octene ≥ 2-octene ≥ 3-octene. The obtained branched poly(2-octene)s and poly(4-octene)s with high molecular weight and Mw/Mn less than 2 were amorphous polymers with low glass transition temperature (Tg) of approximately -66 °C. At 0 °C, 4-octene polymerized in a living/controlled manner. The NMR analyses of the polymers showed that the chain-walking polymerization of 4-octene gave periodically branched polymers with the constant branching density, while that of 2-octene gave the polymer possessing fewer branches than the expected value due to monomer-isomerization. The (n+2),(n+3)- and (n+3),(n+2)-insertions of the internal (n+2)-alkene [CH3(CH2)nCH=CH(CH2)mCH3] followed by chain-walking were confirmed by the 13C NMR analysis of the produced polymers.
- Wang, Fuzhou,Tanaka, Ryo,Li, Qingshan,Nakayama, Yuushou,Shiono, Takeshi
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supporting information
p. 1358 - 1367
(2018/05/23)
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- Room-temperature Suzuki-Miyaura cross-coupling reaction with α-diimine Pd(II) catalysts
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An α-diimine Pd(II) complex containing chiral sec-phenethyl groups, {bis[N,N′-(4-methyl-2-sec-phenethylphenyl)imino]-2,3-butadiene}dichloropalladium (rac-C1), was synthesized and characterized. rac-C1 was applied as an efficient catalyst for the Suzuki-Miyaura cross-coupling reaction between various aniline halides and arylboronic acid in PEG-400-H2O at room temperature. Among a series of aniline halides, rac-C1 did not catalyze the cross-coupling of aniline chlorides and fluorides but efficiently catalyzed the cross-coupling of aniline bromides and iodides with phenylboronic acid. The catalytic activity reduced slightly with increasing steric hindrance of the aniline bromides. The complexes {bis[N,N′-(4-fluoro-2,6-diphenylphenyl)imino]-2,3-butadiene}dichloropalladium and {bis[N,N′-(4-fluoro-2,6-diphenylphenyl)imino]acenaphthene}dichloropalladium were also found to be efficient catalysts for the reaction.
- Wang, Fuzhou,Tanaka, Ryo,Cai, Zhengguo,Nakayama, Yuushou,Shiono, Takeshi
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p. 771 - 776
(2015/11/09)
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- A novel aromatic alkylation of anilines with cyclic and acyclic ketones under hydrothermal conditions
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A novel aromatic ring-alkylation was achieved by condensation between aniline-HCl salts and cyclic or acyclic ketones under hydrothermal conditions.
- Mehta, Barun K.,Kumamoto, Koji,Yanagisawa, Kazumichi,Kotsuki, Hiyoshizo
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p. 6953 - 6956
(2007/10/03)
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- NITROGENOUS HETEROCYCLIC DERIVATIVE HAVING 2,6-DISUBSTITUTED STYRYL
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The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.
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Page/Page column 14
(2010/02/14)
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- Transformation of mutagenic aromatic amines into non-mutagenic species by alkyl substituents: Part I. Alkylation ortho to the amino function
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Alkyl-substituted derivatives of 2-aminonaphthalene (2-AN) 1, 2-aminofluorene (2-AF) 6 and 4-aminobiphenyl (4-ABP) 11 were synthesized and the mutagenic activity of these compounds determined in Salmonella typhimurium strains TA98 and TA100 with and without S9 mix. In the case of the ortho-substituted 4-aminobiphenyls 12-15 (3-alkyl = ethyl, iso-propyl, n-butyl, tert-butyl) the substituent with the strongest steric demand (3-tert-butyl) shows the strongest influence on the decrease of mutagenicity if compared with the parent compound. In the series of the bis-ortho-disubstituted compounds 16-18 (3,5-dimethyl-, 3,5-diethyl- and 3,5-diisopropyl-4-aminobiphenyl) generation of non-mutagenic species occurs already with the introduction of two ethyl groups. For the 4-aminobiphenyl derivatives 12-15 and 16-18, as well as for the 1-alkylated 2-aminofluorenes 7-10 and the 1-alkylated 2-aminonaphthalenes 2-5 a smaller mutagenicity was observed if compared with predicted mutagenicities as calculated by the QSAR equations of Debnath et al. (Environ. Mol. Mutagen. 19 (1992) 37). The largest differences resulted in the cases of the tert-butyl substituted compounds. Only with smaller alkyl groups like ethyl the QSAR predictions and the experimentally determined mutagenicities come close to each other. Thus, these results show that appropriate alkyl substitution reduces (eliminates) mutagenicity, secondly, it is necessary to introduce steric parameters to predict the mutagenicity of such compounds correctly.
- Glende, Carsten,Schmitt, Heimo,Erdinger, Lothar,Engelhardt, Guenter,Boche, Gernot
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- Reactions of Aryl Azides with Alkenes in the Presence of Aluminium Trichloride. Formation of Novel Aziridines fused to Seven- and Eight-membered Rings
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Reactions of aryl azides (1) with cyclohexene gave 3-(arylamino)cyclohexenes (2) and trans-1-chloro-2-(arylamino)cyclohexanes (3), whereas that of (1) with cycloheptene or cis-cyclo-octene afforded novel aziridines, 8-aryl-8-azabicyclooctanes (4), or 9-aryl-9-azabicyclononanes (5), respectively.The reaction of phenyl azide (1a) with cis-4-methylpent-2-ene yielded 3-anilino-2-chloro-4-methylpentane (10), but that with the trans-alkene gave 4-anilino-2-methylpent-2-ene (7) and 3-anilino-4-methylpent-1-ene (8).The similar reaction of (1) with 3-trimethylsilylcyclohexene or 3-trimethylsilyl-cis-cyclo-octene produced only (2) or 3-(arylamino)-cis-cyclo-octenes (2').The formation of the aziridines or the ring-opened products was explained by a mechanism via an aziridinium-AlCl3 complex formed from an azide-AlCl3 complex.
- Takeuchi, Hiroshi,Shiobara, Yukihiko,Kawamoto, Hideyuki,Koyama, Kikuhiko
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p. 321 - 327
(2007/10/02)
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