642477-82-5Relevant academic research and scientific papers
Application of Pd-Catalyzed Cross-Coupling Reactions in the Synthesis of 5,5-Dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles that Inhibit ALK5 Kinase
Tenora, Luká?,Galeta, Juraj,?ezní?ková, Eva,Kry?tof, Vladimír,Potá?ek, Milan
, p. 11841 - 11856 (2016/12/09)
C-H activation of position 3 of a substituted pyrazole ring catalyzed by palladium(II) was straightforward and convenient for arylated or heteroarylated 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. Moreover, we introduced simple protection of the nitrogen in the pyridin-2-yl directing group, which otherwise does not allow a cross-coupling reaction, by transformation to the N-oxide. Selected final products were reasonably selective ALK5 kinase inhibitors.
Flexible palladium-catalysed amidation reactions for the synthesis of complex aryl amides
Barfoot, Christopher,Brooks, Gerald,Brown, Pamela,Dabbs, Steven,Davies, David T.,Giordano, Ilaria,Hennessy, Alan,Jones, Graham,Markwell, Roger,Miles, Timothy,Pearson, Neil,Smethurst, Christian A.
body text, p. 2685 - 2689 (2010/06/21)
This Letter describes the synthesis of complex aryl amides using palladium-catalysed amidation reactions. Use of these conditions allowed for the coupling of a variety of aryl halides and triflates with a host of primary amides in high yields.
Assembly of 4-aminoquinolines via palladium catalysis: A mild and convenient alternative to SNAr methodology
Margolis, Brandon J.,Long, Kimberly A.,Laird, Dana L. T.,Ruble, J. Craig,Pulley, Shon R.
, p. 2232 - 2235 (2007/10/03)
4-Aminoquinolines, classically prepared via SNAr chemistry from an amine and 4-haloquinoline, are important scaffolds in medicinal chemistry. Interest in these compounds prompted us to explore palladium catalysis as an alternative to the existing methods for their preparation. Initial results followed by an iterative screening paradigm confirmed Pd(OAc)2/ DPEphos/K3PO4 as a mild and convenient alternative for the formation of the C-N bond in 4-aminoquinolines. A description of the screen and the scope of this methodology are discussed herein.
ANTIBACTERIAL AGENTS
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Page/Page column 32, (2010/11/25)
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
ANTIBACTERIAL COMPOUNDS
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Page 95, (2008/06/13)
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man
