453560-74-2Relevant articles and documents
Deoxofluorination of (Hetero)aromatic Acids
Alekseenko, Anatoliy N.,Bugera, Maksym Ya.,Gerus, Igor I.,Kiriakov, Oleksandr,Klipkov, Anton A.,Mykhailiuk, Pavel K.,Pustovit, Yurii,Razhyk, Bohdan,Semenov, Sergey,Starova, Viktoriia S.,Tananaiko, Oksana Yu.,Tarasenko, Karen,Tolmachev, Andrei A.,Trofymchuk, Serhii,Zaporozhets, Olga A.
, p. 3110 - 3124 (2020/03/23)
Diverse trifluoromethyl-substituted compounds were synthesized by deoxofluorination of cinnamic and (hetero)aromatic carboxylic acids with sulfur tetrafluoride. The obtained products were used as starting materials in the preparation of novel fluorinated amino acids, anilines, and aliphatic amines - valuable building blocks for medicinal chemistry and agrochemistry.
NOVEL 6-6 BICYCLIC AROMATIC RING SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
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Page/Page column 226, (2017/03/14)
The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1 H -pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase
Talamas, Francisco X.,Abbot, Sarah C.,Anand, Shalini,Brameld, Ken A.,Carter, David S.,Chen, Jun,Davis, Dana,De Vicente, Javier,Fung, Amy D.,Gong, Leyi,Harris, Seth F.,Inbar, Petra,Labadie, Sharada S.,Lee, Eun K.,Lemoine, Remy,Le Pogam, Sophie,Leveque, Vincent,Li, Jim,McIntosh, Joel,Nájera, Isabel,Park, Jaehyeon,Railkar, Aruna,Rajyaguru, Sonal,Sangi, Michael,Schoenfeld, Ryan C.,Staben, Leanna R.,Tan, Yunchou,Taygerly, Joshua P.,Villase?or, Armando G.,Weller, Paul E.
, p. 1914 - 1931 (2014/04/03)
In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we
Trifluoromethylation of arenediazonium salts with fluoroform-derived CuCF3 in aqueous media
Lishchynskyi, Anton,Berthon, Guillaume,Grushin, Vladimir V.
supporting information, p. 10237 - 10240 (2014/08/18)
A new protocol has been developed for trifluoromethylation of arenediazonium salts with moisture-sensitive CuCF3 (from fluoroform) in aqueous media. The reaction is governed by a radical mechanism, tolerates a broad variety of functional groups, and is applicable to the synthesis of complex, polyfunctionalized molecules. This journal is the Partner Organisations 2014.
Conversion of aromatic amino into trifluoromethyl groups through a Sandmeyer-type transformation
Wang, Xi,Xu, Yan,Zhou, Yujing,Zhang, Yan,Wang, Jianbo
supporting information, p. 2143 - 2148 (2014/08/18)
A novel strategy for aromatic trifluoromethylation by converting amino into trifluoromethyl groups via a Sandmeyer-type reaction is reported. The transformation involves diazotization of the aromatic amines with tert-butyl nitrite and hydrochloric acid to form aryldiazonium chlorides, followed by trifluoromethylation with trifluoromethylsilver at low temperature. Various readily available aromatic amines are smoothly converted under mild conditions. Georg Thieme Verlag Stuttgart. New York.
Trifluoromethylation of 1-aryl-3,3-diisopropyltriazenes
Hafner, Andreas,Braese, Stefan
supporting information, p. 996 - 1000 (2013/05/08)
A new method for the trifluoromethylation of functionalized aromatic diisopropyltriazenes is described. In a facile two-step, one-pot synthesis, various functionalized trifluoromethyl-substituted arenes are accessible in mostly good yields by using methyl iodide as iodination agent and the trifluoromethylation system (trifluoromethyl)trimethylsilane/potassium fluoride/copper iodide. This concept could be expanded to perfluoroethylation as well as ethoxycarbonyldifluoromethylation reactions. Copyright
Silver-mediated trifluoromethylation of aryldiazonium salts: Conversion of amino group into trifluoromethyl group
Wang, Xi,Xu, Yan,Mo, Fanyang,Ji, Guojing,Qiu, Di,Feng, Jiajie,Ye, Yuxuan,Zhang, Songnan,Zhang, Yan,Wang, Jianbo
supporting information, p. 10330 - 10333 (2013/08/23)
A novel strategy for aromatic trifluoromethylation by converting aromatic amino group into CF3 group is reported herein. This method, which can be considered as trifluoromethylation variation of the classic Sandmeyer reaction, uses readily available aromatic amines as starting materials and is performed under mild conditions.
HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Page/Page column 42, (2010/12/29)
Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Page/Page column 69; 70, (2010/07/08)
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS
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Page/Page column 64-65, (2010/07/04)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.