- Intensified synthesis of [3,4-d]triazole-fused chromenes, coumarins, and quinolones
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Abstract: Efficient and metal-free synthesis of [3,4-d]triazole-fused chromenes, coumarins, and quinolones has been achieved in an intensified regime using microwave heating. The smooth 1,3-dipolar cycloaddition reaction of heterocyclic nitroalkenes with
- Schwendt, Georg,Glasnov, Toma
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- Direct one-pot synthesis of 3-nitroquinolin-2(1H)-one via H2O/AcOH system: An improvement to classical Friedlander reaction
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Quinolin-2(1H)-ones and their derivatives have attracted considerable attention because of their extensive applications in the field of pharmaceuticals, agricultural and dye chemistry. In contrast to the existed synthetic methods, herein we present the one-pot cascade reaction of 1,1-dimeoxyth-2-nitroethene and 2-aminobenzaldehydes which is catalyst-free and via eco-friendly H2O/AcOH solvent, achieving 3-nitroquinolin-2(1H)-ones in moderate to excellent yields. Importantly, this concise and versatile protocol is a potential improvement to the traditional Friedlander reaction.
- Chen, Xin-fei,Ren, Chao,Xu, Xiao-yong,Shao, Xu-sheng,Li, Zhong
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- Chemodynamic therapy agents Cu(II) complexes of quinoline derivatives induced ER stress and mitochondria-mediated apoptosis in SK-OV-3 cells
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Three Cu(II) complexes of quinoline derivatives as cancer chemodynamic therapy agents were synthesized and characterized. These complexes were heavily taken up by cells and reacted with cellular glutathione (GSH) to reduce Cu2+ to Fenton-like C
- Chen, Zhen-Feng,Jia, Chun-Peng,Liang, Hong,Mo, An-Na,Shen, Wen-Ying
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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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