591754-12-0Relevant articles and documents
Efficient and Mild Ullmann-Type N-Arylation of Amides, Carbamates, and Azoles in Water
Bollenbach, Maud,Aquino, Pedro G. V.,de Araújo-Júnior, Jo?o Xavier,Bourguignon, Jean-Jacques,Bihel, Frédéric,Salomé, Christophe,Wagner, Patrick,Schmitt, Martine
supporting information, p. 13676 - 13683 (2017/10/10)
A simple, sustainable, efficient, mild, and low-cost protocol was developed for d-glucose-assisted Cu-catalyzed Ullmann reactions in water for amides, carbamates, and nitrogen-containing heterocycles. The reaction was compatible with diverse aryl/heteroaryl iodides, giving highly substituted pyridine, indole, or indazole rings. This method offers an attractive alternative to existing protocols, because the reaction proceeds in aqueous media, occurs at or near ambient temperature, and provides the N-arylated products in good to high yields.
Amide-based inhibitors of p38α MAP kinase. Part 1: Discovery of novel N-pyridyl amide lead molecules
Luedtke, Gregory R.,Schinzel, Kurt,Tan, Xuefei,Tester, Richland W.,Nashashibi, Imad,Xu, Yong-jin,Dugar, Sundeep,Levy, Daniel E.,Jung, Joon
scheme or table, p. 2556 - 2559 (2010/07/03)
A novel series of N-pyridyl amides as potent p38α kinase inhibitors is described. Based on the structural similarities between the initial hit and a well-known imidazole pyrimidine series of p38α inhibitors, potencies within the newly discovered series were quickly improved by installation of an (S)-α-methylbenzyl moiety at the 2-position of the pyridine ring. The proposed binding modes of the new series to p38α were evaluated against SAR findings and provided rationale for further development of this series of molecules.
2,4-Disubstituted pyrimidines: A novel class of KDR kinase inhibitors
Manley, Peter J.,Balitza, Adrienne E.,Bilodeau, Mark T.,Coll, Kathleen E.,Hartman, George D.,McFall, Rosemary C.,Rickert, Keith W.,Rodman, Leonard D.,Thomas, Kenneth A.
, p. 1673 - 1677 (2007/10/03)
2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC50=105 nM, Cell IC50=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative 2d (KDR IC50=6 nM, cell IC50=19 nM).
