20849-26-7Relevant academic research and scientific papers
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors
Haffner, Curt D.,Charnley, Adam K.,Aquino, Christopher J.,Casillas, Linda,Convery, Máire A.,Cox, Julie A.,Elban, Mark A.,Goodwin, Nicole C.,Gough, Peter J.,Haile, Pamela A.,Hughes, Terry V.,Knapp-Reed, Beth,Kreatsoulas, Constantine,Lakdawala, Ami S.,Li, Huijie,Lian, Yiqian,Lipshutz, David,Mehlmann, John F.,Ouellette, Michael,Romano, Joseph,Shewchuk, Lisa,Shu, Arthur,Votta, Bartholomew J.,Zhou, Huiqiang,Bertin, John,Marquis, Robert W.
supporting information, p. 1518 - 1523 (2019/10/19)
Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2). Fragment based screening and design principles led to the identification of the inhibitor series, and X-ray crystallography was used to inform key structural changes. Through key substitutions about the N1 and C5 N positions on the pyrazole ring significant kinase selectivity and potency were achieved. Bridged bicyclic pyrazolocarboxamide 11 represents a selective and potent inhibitor of RIP2 and will allow for a more detailed investigation of RIP2 inhibition as a therapeutic target for autoinflammatory disorders.
A facile synthesis of trifluoromethyl- and 3,3,3-trifluoropropenyl- substituted aromatic compounds by the oxidative desulfurization-fluorination of the corresponding carbodithioates
Furuta, Satoru,Kuroboshi, Manabu,Hiyama, Tamejiro
, p. 805 - 819 (2007/10/03)
Trifluoromethyl-substituted aromatic compounds were easily synthesized by the oxidative desulfurization-fluorination reaction of readily accessible methyl arenecarbodithioates using [n-Bu4N]H2F3 and 1,3-dibromo-5,5- dimethylhydantoin (DBH) under extremely mild conditions. Use of N- bromosuccinimide or N-iodosuccinimide instead of DBH afforded difluoro(methylthio)methyl-substituted aromatics. In a similar way, 3,3,3- trifluoropropenyl-substituted aromatic compounds were readily prepared from the corresponding α,β-unsaturated carbodithioates.
ELEKTROCHEMISCHE OXIDATION VON DITHIOCARBONSAEUREESTERN ZU ISOTHIAZOLEN
Voss, Juergen,Mischke, Peter,Adiwidjaja, Gunadi
, p. 261 - 274 (2007/10/02)
Electrolysis of alkyl arenedithioates 1 in acetonitrile with benzyl-triethyl-ammonium chloride as supporting electrolyte yields 5-aryl-4-cyano-3-methyl-isothiazoles 4.A reaction path is discussed according to which the dithioesters 1 are chlorinated at the anode and subsequently react with 3-iminobutyronitrile (6), generated at the cathode, to form the isothiazoles 4.
