652153-62-3Relevant academic research and scientific papers
Ligand-Promoted Meta-C-H Arylation of Anilines, Phenols, and Heterocycles
Wang, Peng,Farmer, Marcus E.,Huo, Xing,Jain, Pankaj,Shen, Peng-Xiang,Ishoey, Mette,Bradner, James E.,Wisniewski, Steven R.,Eastgate, Martin D.,Yu, Jin-Quan
supporting information, p. 9269 - 9276 (2016/08/05)
Here we report the development of a versatile 3-acetylamino-2-hydroxypyridine class of ligands that promote meta-C-H arylation of anilines, heterocyclic aromatic amines, phenols, and 2-benzyl heterocycles using norbornene as a transient mediator. More than 120 examples are presented, demonstrating this ligand scaffold enables a wide substrate and coupling partner scope. Meta-C-H arylation with heterocyclic aryl iodides as coupling partners is also realized for the first time using this ligand. The utility for this transformation for drug discovery is showcased by allowing the meta-C-H arylation of a lenalidomide derivative. The first steps toward a silver-free protocol for this reaction are also demonstrated.
Amination of aryl iodides using a fluorous-tagged ammonia equivalent
Nielsen, Simon Dalsgaard,Smith, Garrick,Begtrup, Mikael,Kristensen, Jesper L.
experimental part, p. 3704 - 3710 (2010/09/05)
A fluorous-tagged ammonia equivalent for the Cu-catalyzed amination of aryl iodides is described in which N-Boc-protected anilines are produced in high overall yield and purity. All purification steps are performed using Fluorous SolidPhase Extraction (F-SPE) greatly simplifying and speeding up the isolation of the desired products.
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors
Kuo, Gee-Hong,DeAngelis, Alan,Emanuel, Stuart,Wang, Aihua,Zhang, Yan,Connolly, Peter J.,Chen, Xin,Gruninger, Robert H.,Rugg, Catherine,Fuentes-Pesquera, Angel,Middleton, Steven A.,Jolliffe, Linda,Murray, William V.
, p. 4535 - 4546 (2007/10/03)
On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a moderately potent cyclin dependent kinase (CDK) inhibitor. A proposed combination of CGP-60474 and
SUBSTITUTED TRIAZINE KINASE INHIBITORS
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Page 41-43, (2010/11/30)
The present invention provides substituted 1,3,5-triazine compounds as kinase inhibitors and a method for treating or ameliorating a kinase mediated disorder.
