1146413-08-2Relevant academic research and scientific papers
Ru(II)-Catalyzed Amination of Aryl Fluorides via η6-Coordination
Kang, Qi-Kai,Li, Yuntong,Lin, Yunzhi,Shi, Hang
supporting information, p. 3706 - 3711 (2020/03/11)
We developed a Ru/hemilabile-ligand-catalyzed nucleophilic aromatic substitution (SNAr) of aryl fluorides as the limiting reagents. Significant ligand enhancement was demonstrated by the engagement of both electron-rich and neutral arenes in the SNAr amination without using excess arenes. Preliminary mechanistic studies revealed that the nucleophilic substitution proceeds on a η6-complex of the Ru catalyst and the substrate, and the hemilabile ligand facilitates dissociation of products from the metal center.
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 1441; 1444; 1445, (2019/02/13)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
4-BENZ0YL-1-SUBSTITUTED-PIPERAZIN-2-0NE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 89, (2009/05/28)
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: A is C1-6alkyl, C3-6cycloalkyl, -CH2-R6, -CHMe-R7, -CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, -CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9; and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, -CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, -CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides the use of the compound or salt for the manufacture of a medicament for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.
