41242-35-7Relevant 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.
N-Bu4NI-catalyzed selective dual amination of sp3 C-H bonds: Oxidative domino synthesis of imidazo[1,5-c]quinazolines on a gram-scale
Zhao, Dan,Wang, Teng,Shen, Qi,Li, Jian-Xin
supporting information, p. 4302 - 4304 (2014/04/17)
An n-Bu4NI catalyzed domino reaction that involves selective dual amination of sp3 C-H bonds has been developed. The protocol affords a facile and efficient approach to the synthesis of imidazo[1,5-c] quinazolines under mild conditions.
Synthesis of 4-quinolones via cyclocondensation of substituted ortho-amidoacetophenones: A refit to the camps cyclization by applying trimethylsilyl trifluoromethanesulfonate/triethylamine
Eidamshaus, Christian,Triemer, Therese,Reissig, Hans-Ulrich
supporting information; experimental part, p. 3261 - 3266 (2011/11/30)
A modification of the classical Camps cyclization is described. A series of substituted 4-quinolone derivatives is prepared via trimethylsilyl trifluoromethanesulfonate/triethylamine induced cyclocondensation of substituted ortho-amidoacetophenones. The process shows a broad substrate scope and allows selective preparation of 2-aryl- and 2-alkyl-substituted 4-quino-lones. Enantiopure starting materials react without loss of optical purity using the modified conditions. Subsequent transformations of the products involving preparation of a 4-quinolyl nonaflate and O-selective methylation are also described. Georg Thieme Verlag Stuttgart · New York.
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.
4(1H)-quinolone derivatives
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, (2008/06/13)
Quinolone derivatives having a quinolone structure: STR1 where Yo is O or S are disclosed, which are useful as cardiotonic agents. Typical examples of the quinolone derivatives include: 6,7-dimethoxy-4 (1H) quinolone (compound 6) and 5-hydroxy-6-methoxy-4(1H) quinolone (compound 1) as typical compounds of the formulae[I] and [I'], respectively, shown in the specification.
