122172-22-9Relevant academic research and scientific papers
Synthesis and anticancer evaluation of 3-substituted quinolin-4-ones and 2,3-dihydroquinolin-4-ones
Rajput, Santosh,Gardner, Christopher R.,Failes, Timothy W.,Arndt, Greg M.,Black, David Stc.,Kumar, Naresh
, p. 105 - 115 (2014/01/17)
A series of 3-aryl-5,7-dimethoxyquinolin-4-ones 8 and 3-aryl-5,7-dimethoxy- 2,3-dihydroquinolin-4-ones 13 were synthesized in good yields. Demethylation under a range of conditions afforded the corresponding 5-hydroxy and 5,7-dihydroxy derivatives. Biolog
Lewis base catalyzed asymmetric hydrosilylation of α-substituted β-enamino esters: Facile access to enantioenriched β2-amino esters via dynamic kinetic resolution
Shu, Chang,Hu, Xiao-Yan,Li, Shuai-Shuai,Yuan, Wei-Cheng,Zhang, Xiao-Mei
supporting information, p. 1879 - 1882 (2014/08/18)
A chiral Lewis base organocatalyzed asymmetric hydrosilylation of α-substituted β-enamino esters is presented. The reactions proceeded through dynamic kinetic resolution to afford various enantioenriched β2-amino esters with high yields (up to
Facile synthesis of highly substituted 2-pyrone derivatives via a tandem Knoevenagel condensation/lactonization reaction of β-formyl-esters and 1,3-cyclohexadiones
Moghaddam, Firouz Matloubi,Mirjafary, Zohreh,Javan, Marjan Jebeli,Motamen, Sara,Saeidian, Hamid
, p. 2908 - 2911 (2014/05/06)
A mild and efficient tandem process for the synthesis of new highly substituted 2-pyrones starting from commercially available 2-arylacetic acids has been developed. The synthesis is based on the Knoevenagel condensation of 1,3-cyclohexadiones with various β-formyl-esters, followed by lactonization in the presence of nano ZnO (20 mol %). Moderate to high yields and readily available cheap starting materials are the key features of the present method.
Imidazonaphthyridine systems (part 2): Functionalization of the phenyl ring linked to the pyridine pharmacophore and its replacement by a pyridinone ring produces intriguing differences in cytocidal activity
Masurier, Nicolas,Debiton, Eric,Jacquemet, Alicia,Bussière, Antoine,Chezal, Jean-Michel,Ollivier, Anthony,Tétégan, Daté,Andaloussi, Mounir,Galmier, Marie-Joseph,Lacroix, Jacques,Canitrot, Damien,Teulade, Jean-Claude,Gaudreault, René C.,Chavignon, Olivier,Moreau, Emmanuel
scheme or table, p. 137 - 150 (2012/07/16)
We recently discovered that five- and pseudo-five-fused-ring derivatives in an imidazonaphthyridine series were promising hit compounds for the development of new DNA-intercalators. In this study, novel (dihydro)imidazo[1,6] and [1,7]naphthyridi(no)nes were prepared including pseudo-pentacycles. All the compounds synthesized were screened against four tumor cell lines. Compounds 3(b-d) showed significant in vitro cytotoxicity, and DNA intercalation properties were demonstrated at 25 μM. Imidazonaphthyridinones exhibited no DNA binding affinity despite significant growth inhibition activity. Interestingly, when a pyridinone pharmacophore was linked to the imidazo[1,2-a]pyridine scaffold, the geometric orientation of the link had a strong impact on the growth inhibition activity. From these results we conclude that the moderate cytotoxicity observed for these compounds is independent of their DNA-binding and topoisomerase inhibition activities.
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials
Snyder, Lawrence B.,Meng, Zhaoxing,Mate, Robert,D'Andrea, Stanley V.,Marinier, Anne,Quesnelle, Claude A.,Gill, Patrice,Den Bleyker, Kenneth L.,Fung-Tomc, Joan C.,Frosco, MaryBeth,Martel, Alain,Barrett, John F.,Bronson, Joanne J.
, p. 4735 - 4739 (2007/10/03)
A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp3-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described.
Venlafaxine production process
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, (2008/06/13)
A process for the preparation of venlafaxin and/or the physiologically acceptable addition salts thereof that consists of reacting a compound of general formula (II) where R is a C1-C10alkyl, aryl, aralkyl or cycloalkyl group of 3 to 6 atoms of carbon, with a organomagnesium compound of general formula (III) where X is an atom of halogen and, if desired, a salt of the thus obtained venlafaxin is formed by reaction thereof with a physiologically acceptable acid.
Enantioselective Robinson Annulation: Synthesis of (+)-O-Methyljoubertiamine
Taber, Douglass F.,Mack, James F.,Rheingold, Arnold L.,Geib, Steven J.
, p. 3831 - 3836 (2007/10/02)
The α-formyl ester derived from 2-(1-naphthyl)-3-borneol, as the potassium salt in moist dimethoxymethane, adds to methyl vinyl ketone to give two adducts in a ratio of 95:5.The relative configuration of the major diastereomer has been confirmed by X-ray crystallography.This diastereomer is readily carried on to (+)-O-methyljoubertiamine.The addition of such naphthylbornyl esters to Michael acceptors should constitute a general laboratory-scale procedure for the enantioselective construction of enantiomerically pure quaternary stereogenic centers.
