234766-97-3Relevant academic research and scientific papers
Modular Synthesis of Di- A nd Trisubstituted Imidazoles from Ketones and Aldehydes: A Route to Kinase Inhibitors
De Toledo, Ian,Grigolo, Thiago A.,Bennett, James M.,Elkins, Jonathan M.,Pilli, Ronaldo A.
, p. 14187 - 14201 (2019/10/16)
A one-pot and modular approach to the synthesis of 2,4(5)-disubstituted imidazoles was developed based on ketone oxidation, employing catalytic HBr and DMSO, followed by imidazole condensation with aldehydes. This methodology afforded twenty-nine disubstituted NH-imidazoles (23%-85% yield). A three-step synthesis of 20 kinase inhibitors was achieved by employing this oxidation-condensation protocol, followed by bromination and Suzuki coupling in the imidazole ring to yield trisubstituted NH-imidazoles (23%-69%, three steps). This approach was also employed in the synthesis of known inhibitor GSK3037619A.
Novel Heterocyclic Compounds and Uses Thereof
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Paragraph 0310, (2013/08/28)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
RAF KINASE INHIBITORS
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Page/Page column 71, (2011/08/03)
Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
NOVEL HETEROCYCLIC COMPOUNDS AND USES THEROF
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Page/Page column 89, (2009/10/22)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Diversity synthesis via C-H bond functionalization: Concept-guided development of new C-arylation methods for imidazoles
Sezen, Bengue,Sames, Dalibor
, p. 10580 - 10585 (2007/10/03)
Herein, we have formulated the concept of systematic derivatization of a structural motif via C-H bond functionalization. This concept may not only serve as a blueprint for new strategies in diversity synthesis but also provide systematic guidance for the
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase
Liverton, Nigel J.,Butcher, John W.,Claiborne, Christopher F.,Claremon, David A.,Libby, Brian E.,Nguyen, Kevin T.,Pitzenberger, Steven M.,Selnick, Harold G.,Smith, Garry R.,Tebben, Andrew,Vacca, Joseph P.,Varga, Sandor L.,Agarwal, Lily,Dancheck, Kim,Forsyth, Amy J.,Fletcher, Daniel S.,Frantz, Betsy,Hanlon, William A.,Harper, Coral F.,Hofsess, Scott J.,Kostura, Matthew,Lin, Jiunn,Luell, Sylvie,O'Neill, Edward A.,Orevillo, Chad J.,Pang, Margaret,Parsons, Janey,Rolando, Anna,Sahly, Yousif,Visco, Denise M.,O'Keefe, Stephen J.
, p. 2180 - 2190 (2007/10/03)
Novel potent and selective diarylimidazole inhibitors of p38 MAP (mitogen-activated protein) kinase are described which have activity in both cell-based assays of tumor necrosis factor-α (TNF-α) release and an animal model of rheumatoid arthritis. The SAR
