955405-13-7Relevant academic research and scientific papers
C-2 phenyl replacements to obtain potent quinoline-based Staphylococcus aureus NorA inhibitors
Astolfi, Andrea,Barreca, Maria Letizia,Biavasco, Francesca,Cannalire, Rolando,Cecchetti, Violetta,Cedraro, Nicholas,Felicetti, Tommaso,Manfroni, Giuseppe,Mangiaterra, Gianmarco,Massari, Serena,Pietrella, Donatella,Sabatini, Stefano,Tabarrini, Oriana
, p. 584 - 597 (2020/02/15)
NorA is the most studied efflux pump of Staphylococcus aureus and is responsible for high level resistance towards fluoroquinolone drugs. Although along the years many NorA efflux pump inhibitors (EPIs) have been reported, poor information is available ab
Selective Oxidative Decarbonylative Cleavage of Unstrained C(sp3)-C(sp2) Bond: Synthesis of Substituted Benzoxazinones
Verma, Ajay,Kumar, Sangit
supporting information, p. 4388 - 4391 (2016/10/11)
A transition metal (TM)-free practical synthesis of biologically relevant benzoxazinones has been established via a selective oxidative decarbonylative cleavage of an unstrained C(sp3)-C(sp2) bond employing iodine, sodium bicarbonate, and tbutyl hydroperoxide in DMSO at 95 °C. Control experiments and Density Functional Theory (DFT) calculations suggest that the reaction involves a [1,5]H shift and extrusion of CO gas as the key steps. The extrusion of CO has also been established using PMA-PdCl2.
Sequential Cu-catalyzed amidation-base-mediated camps cyclization: A two-step synthesis of 2-aryl-4-quinolones from o-halophenones
Jones, Carrie P.,Anderson, Kevin W.,Buchwald, Stephen L.
, p. 7968 - 7973 (2008/02/13)
(Chemical Equation Presented) A direct two-step method for the preparation of 2-aryl- and 2-vinyl-4-quinolones that utilizes a copper-catalyzed amidation of o-halophenones followed by a base-promoted Camps cyclization of the resulting N-(2-ketoaryl)amides is described. With CuI, a diamine ligand, and base as the catalyst system, the amidation reactions proceed in good yields for a range of aryl, heteroaryl, and vinyl amides. The subsequent Camps cyclization efficiently provides the desired 4-quinolones with the conditions that are described.
