Bromine–magnesium exchange using iPrMgCl in THF at room temperature on 2-, 3- and 4-bromopyridines allowed the synthesis of various functionalized pyridines. The methodology was successfully used for the synthesis of 4-azaxanthone. Moreover, single exchange reactions observed on 2,6-, 3,5-, 2,3...
The synthesis of original imidazo[1,2-a]pyridines bearing a thioether side chain at the 3 position and diversely substituted on the 6 or 8 position, and their antiviral activities are reported. From the synthesized compounds, the imidazo[1,2-a]pyridines bearing a 5 membered heterocycle (thiophen...
A series of 26 bis(arylimino)pyridine iron(III) complexes containing either electron withdrawing or electron donating substituents in their ligand frameworks was synthesized and characterized. After activation with methylaluminoxane (MAO), these catalysts oligomerize or polymerize ethylene to gi...
Sequential radical addition/5-exo-cyclization/β-elimination reactions, accomplished by thermally or photolytically induced decompositions of O-acyl derivatives of N-hydroxypyridine-2-thione or other thiohydroxamic esters of 6-phenylthio-4-hexenoic acid 11 in the presence of an excess of radicop...
A series of 5,6-disubstituted pyridine-2,3-dione-3-thiosemicarbazone derivatives(2a-2n) and 5,6-disubstituted pyridine-2,3-dione S-benzyl-3-thiosemicarbazones(3a-3g) were synthesized starting from 2,3-dihydroxypyridine via oxidation-Michael additions, condensations and nucleophilic substitutions...
Ring-opened benzothieno[3,2-b]quinolinium salts (3) were designed and synthesized with substitution on the thiophene moiety. In vitro screenings were carried out against fungal pathogens including Cryptococcus neoformans, Candida albicans, Candida glabrata, Candida krusei and Aspergillus fumigat...
A general and simple synthesis of 2,4,6-trisubstituted pyridines and fused pyridine-2-ones from bromoacetic acid is developed via a DMAP-promoted in situ activation strategy. In this protocol, readily accessible bromoacetic acid has been effectively employed as a 2C synthon to undergo formal [2+...
A series of 2,3-disubstituted pyridines were synthesized as potential non-emetic PDE4 inhibitors. To decrease brain exposure and minimize emesis, we modified the lipophilic moiety of a series of emetic PDE4 inhibitors and found that introduction of a hydroxy group into the pyridine moiety of the...
In this work, an efficient copper-catalyzed three-component reaction for the synthesis of sulfenylimidazo[1,2-a]pyridines using elemental sulfur as the sulfenylating agents has been developed. The reaction could proceed smoothly with a high degree of functional group tolerance and provide the de...
The asymmetric cyclopropanation of vinylphosphonate using (S)-dimethylsulfonium-(p-tolylsulfinyl)methylide was applied to obtain a dideuterated cyclopropyl sulfoxide. A three-step synthesis of enantiopure (+)-(1R)-1-amino-2,2-dideuteriocyclopropanephosphonic acid (+)-17-d2 was developed.
We describe herein a new synthesis of enantiopure alkylidene 1,1-bis-p-tolyl-sulfoxides (5), based on a two-steps sequence. The first one involves the alkylation of the lithium anion of the (S,S)-bis-p-tolylsulfinylmethane (1) with aldehydes. The second one consists in a mild dehydration of the ...
Functionalized 1-azaxanthones (5-oxo-5H-[1]-benzopyrano[2,3-b]pyridines) were prepared by TMSOTf-mediated condensation of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with 3-cyanochromones and subsequent base-mediated domino ‘retro-Michael/nitrile-addition/heterocyclization’ reaction.
3-Hydroxy-4-alkoxycarbonyl-butenolides were prepared by one-pot cyclizations of 1,3-bis(silyloxy)alk-1-enes with oxalyl chloride.
The thermal behavior, mechanism and kinetic parameters of the exothermic first-stage decomposition reaction of the title compound in a temperature-programmed mode have been investigated by means of DSC, TG-DTG and IR. The reaction mechanism was proposed. The kinetic model function in differentia...
3,3′-(1,2-ethanediyl)bis[2-substituted-1,3-thiazolidin-4-one] derivatives display different biological activities depending on the configuration of the 2,2′ centers and on the substitution at C2, C2′. In this context, 3,3′-(1,2-ethanediyl)bis[2-(2′-(5′-methyl)thienyl)-1,3-thiazolidin-4-one...
The antibacterial activity and mechanism of 2R,3R-dihydromyricetin (DMY) against Staphylococcus aureus were investigated. The minimum inhibitory concentration of DMY against S. aureus was 0.125 mg/ml, and the growth inhibitory assay also revealed that DMY showed a potent antibacterial activity a...
Synthesis, characterization and mesomorphic properties of dpyp-linked dicobaloxime of the kind [C15H31-CH2Co(dmgH)2]2-µ-1,3-bis(4-pyridyl)propane has been reported. This cobaloxime complex was characterized by UV-visible and Fourier Transform Infrared spectroscopy, 1H and 13C nuclear magnetic r...
The present work describes the application of high-speed counter-current chromatography to the preparative separation of a previously unreported impurity in the color additive D&C Red No. 17 (R17, Colour Index No. 26100, Sudan III). Due to the hydrophobic nature of the impurity, a hydrophobic tw...
The bis(trifluoromethylsulfonyl)imide anion (TFSI) is one of the common anions forming hydrophobic ionic liquids at room temperature. In this work, through an introduction of two carboxyl groups into the imidazolium cation, a hydrophilic 1,3-bis(carboxymethyl)imidazolium bis(trifluoromethylsulfo...
A series of new squaraine dyes was synthesized by the condensation of 1,2-dihydroxycyclobuten-3,4-dione with various p-substituted anilines. The spectroscopic properties of these compounds were studied in ten solvents exhibiting different polarity. The solvatochromism of 1,3-bis(p-substituted ph...
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