- Copper-Catalyzed Amination of C(sp3)-H bonds: From Anilides to Indolines
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Copper-catalyzed oxidative intramolecular cyclization of o-alkylated anilines via cleavage of C(sp3)-H and N-H bonds for the production of indolines is described. This approach provides a straightforward strategy for the synthesis of nitrogen-c
- Long, Jinguo,Le, Liyuan,Iwasaki, Takanori,Qiu, Renhua,Kambe, Nobuaki
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p. 482 - 492
(2019/12/24)
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- 2,3-DIHYDROQUINAZOLIN COMPOUNDS AS NAV1.8 INHIBITORS
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The present invention relates to Nav1.8 Inhibitor 2,3-dihydroquinazolin compounds of Formula (X); wherein Y', X', B', R1', R2', R3', R5', R6', R7', and z1 are as defined herein; or pharmaceutically acceptable salts or tautomer forms thereof, corresponding pharmaceutical compositions or formulations, methods or processes of compound preparation, methods, compounds for use in, uses for and/or combination therapies for treating pain and/or pain-related or associated disease(s), disorder(s) or condition(s), respectively.
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Page/Page column 161; 198
(2021/01/23)
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- POLYCYCLIC COMPOUND AND AN ORGANIC ELECTROLUMINESCENCE DEVICE COMPRISING THE POLYCYCLIC COMPOUND OR THE COMPOSITION
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Specific polycyclic compounds, a material for an organic electroluminescence device comprising said specific polycyclic compound, an organic electroluminescence device comprising said specific polycyclic compound, an electronic equipment comprising said organic electroluminescence device, a process for preparing said polycyclic compounds, and the use of said polycyclic compounds in an organic electroluminescence. (Formula I) (I)
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Page/Page column 303-304
(2020/11/03)
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- Air-stable Bis(pentamethylcyclopentadienyl) Zirconium Perfluorooctanesulfonate as an Efficient and Recyclable Catalyst for the Synthesis of N-substituted Amides
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Bis(pentamethylcyclopentadienyl) zirconium perfluorooctanesulfonate is an air-stable and water-tolerant Lewis acid. This complex exhibited good thermal stability and high solubility in polar organic solvents. The compound showed relatively strong acidity, with an acid strength of 0.8Ho≤3.3, and high catalytic efficiency for the synthesis of N-substituted amides via the reaction of carboxylic acids with amines, the Ritter reaction of nitriles with alcohols, and the amination of alcohols with amides. Moreover, the complex had good reusability. This catalytic system affords a simple and efficient way to synthesize N-substituted amides.
- Li, Ningbo,Wang, Lingxiao,Zhang, Liting,Zhao, Wenjie,Qiao, Jie,Xu, Xinhua,Liang, Zhiwu
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p. 3532 - 3538
(2018/08/01)
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- Sulfated choline ionic liquid-catalyzed acetamide synthesis by grindstone method
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Sulfated choline ionic liquid (SCIL) has been found to be an efficient solid acid IL catalyst for the protection of amine groups with acetic anhydride under solvent-free grindstone conditions. The attractive features of this new catalytic methodology include its sustainability, facile work-up procedure, economic viability, and biodegradability. The SCIL catalyst was characterized using infrared spectroscopy, wide-angle X-ray scattering analysis, and scanning electron microscopy with energy dispersive X-ray spectroscopy. The catalyst could be reused six times without significant loss in activity. Furthermore, no chromatographic separations were needed to obtain the desired products.
- Kalla, Reddi Mohan Naidu,Lim, Jaehwa,Bae, Jaeyeong,Kim, Il
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supporting information
p. 1595 - 1599
(2017/04/03)
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- Cu-Catalyzed Intramolecular Amidation of Unactivated C(sp3)-H Bonds to Synthesize N-Substituted Indolines
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A copper-catalyzed intramolecular amidation of unactivated C(sp3)-H bonds to construct indoline derivatives has been developed. Such an amidation proceeded well at primary C-H bonds preferred to secondary C-H bonds. The transformation owned a b
- Pan, Fei,Wu, Bin,Shi, Zhang-Jie
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supporting information
p. 6487 - 6490
(2016/05/02)
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- Catalytic C(sp3)?H Arylation of Free Primary Amines with an exo Directing Group Generated In Situ
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Herein, we report the palladium-catalyzed direct arylation of unactivated aliphatic C?H bonds in free primary amines. This method takes advantage of an exo-imine-type directing group (DG) that can be generated and removed in situ. A range of unprotected aliphatic amines are suitable substrates, undergoing site-selective arylation at the γ-position. Methyl as well as cyclic and acyclic methylene groups can be activated. Furthermore, when aniline-derived substrates were used, preliminary success with δ-C?H arylation was achieved. The feasibility of using the DG component in a catalytic fashion was also demonstrated.
- Xu, Yan,Young, Michael C.,Wang, Chengpeng,Magness, David M.,Dong, Guangbin
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supporting information
p. 9084 - 9087
(2016/07/26)
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- DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
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The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
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Page/Page column 57
(2012/04/04)
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- Pharmaceutical/cosmetic compositions comprising novel ligands that activate RAR receptors
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Novel ligand compounds that activate RAR receptors have the following structural formula (I): and are suited for formulation into pharmaceutical compositions useful in human or veterinary medicine, or, alternatively, into cosmetic compositions.
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Page/Page column 9
(2010/11/25)
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- Cinnamide and hydrocinnamide derivatives with kinase inhibitory activity
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The present invention provides novel cinnamide compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
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Page/Page column 137
(2008/06/13)
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- A chiral axis due to an acyclic imide-Ar bond: A study of steric effects of acyl groups on racemization
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Studies on the racemization in a series of optically active compounds 3a-e, including the steric effect of their acyl groups, are described. The first example of optically active compounds 3c and 3d, which possess axial chirality based on an acyclic imide-Ar bond, has been reported. A quite interesting result has been revealed, namely, that 3a bearing a bulky acyl group rather than a relatively small one racemized more easily. To explain this observed phenomenon, 13C NMR experiments and the reaction with benzylamine of 3a-e were undertaken. These results suggested that the t-BuCO-N bond in 3a which racemized easily, is more twisted, compared with the RCO-N bonds in 3b-e which are relatively stable to racemization. Furthermore, the absolute configuration of 3b and 3c has been determined to be R by the CD spectrum and the X-ray crystallographic analysis of racemic 3f has been accomplished. (C) 2000 Published by Elsevier Science Ltd.
- Kondo, Kazuhiro,Iida, Takeko,Fujita, Hiroko,Suzuki, Tomoko,Yamaguchi, Kentaro,Murakami, Yasuoki
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p. 8883 - 8891
(2007/10/03)
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- 3,5-Di-t-butylnitrosobenzene as a spin trap for N-arylamidyl free radicals
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Acyl- and benzenesulphonyl-anilines with one or two t-butyl groups in ortho positions generate transient amidyl radicals, which were evidenced by traping with 3,5-di-t-butylnitrosobenzene.Spectral simulation showed the simultaneous presence of two paramag
- Bologa, U. L.,Oniciu, D. C.,Ciureanu, M.,Barsan, F.,Ghiviriga, I.,Balaban, A. T.
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