- An improved method for the synthesis of 3-amino-1H-quinolin-2-one
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An efficient method for the synthesis of 3-amino-1H-quinolin-2-one is described. Condensation of o-nitrobenzaldehyde with hippuric acid gave 4-(2-nitrobenzylidene)-2-phenyloxazol-5-one. This compound was reduced to give 4-(2-aminobenzylidene)-2-phenyloxaz
- Juarez-Gordiano, Cecilia,Hernandez-Campos, Alicia,Castillo, Rafael
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- An expeditious copper-catalyzed access to 3-aminoquinolinones, 3-aminocoumarins and anilines using sodium azide
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An efficient copper-catalyzedin in situ C-(sp2)-NH2 bond formation to provide a range of 3-aminoquinolin-2(1H)-ones and 3-aminocoumarins from 3-bromoquinolinones and 3-bromocoumarins, respectively, has been achieved. The reaction conditions involve the use of copper powder as the catalyst, eco-friendly ethanol as the solvent in the pres ence of pipecolinic acid as the ligand and ascorbic acid as the additive. The efficiency of this practical method was demonstrated in the synthesis of various anilines.
- Messaoudi, Samir,Brion, Jean-Daniel,Alami, Mouad
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experimental part
p. 1677 - 1687
(2010/10/01)
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- Synthesis of 4-(2-chloroethyl)-2,3-dihydro[1,4]oxazino[2,3-b]quinoline and 4-(2-chloroethyl)-2,3-dihydropyrido[2,3-b][1,4]oxazine
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The title compounds were synthesized from 3-[bis(2- hydroxyethyl)amino]quinolin-2(1H)-one 11a and 3-[bis(2- hydroxyethyl)amino]pyridin-2(1H)-one 18 respectively. The preparation involved a tandem chlorination/cyclization reaction.
- Anderson,Dalvie
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p. 1533 - 1536
(2007/10/02)
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- Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one
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A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
- Saari, Walfred S.,Wai, John S.,Fisher, Thorsten E.,Thomas, Craig M.,Hoffman, Jacob M.,et al.
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p. 3792 - 3802
(2007/10/02)
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- Cardiotonic Agents. 1. Synthesis and Structure-Activity Relationships in a New Class of 3-,4-, and 5-Pyridyl-2(1H)-quinolone Derivatives
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A series of 3-,4-, and 5-pyridyl-2(1H)-quinolone derivatives with H or HO or CH3O substituents in the 8-position were prepared and tested for positive inotropic activity.Several derivatives, especially 29, 9b, and 27 with a pyridyl ring in the 5-position,
- Leclerc, Gerard,Marciniak, Gilbert,Decker, Nicole,Schwartz, Jean
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p. 2427 - 2432
(2007/10/02)
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- 2-METHYL-4-(o-NITROBENZYLIDENE)OXAZOL-5-ONES
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The cis and trans isomers of 2-methyl-4-(o-nitrobenzylidene)oxazol-5-one have been obtained.On reduction, the cis isomer formed 3-acetamidoquinolin-2-ol, and the trans isomer formed 4-(o-aminobenzylidene)-2-methyloxazol-5-one.Details of the IR, UV, PMR, a
- Mazurov, A. A.,Andronati, S. A.,Antonenko, V. V.
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p. 514 - 515
(2007/10/02)
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