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Condensation of 2-chloro- and 2,3-dichloroquinoxalines with alk-1-ynes in the presence of bis(triphenylphosphine)palladium(II) dichloride and copper(I) iodide gives mono- and di-alkynylquinoxalines.Addition of amines to these products gives stable enamines; hydration gives 2′-oxoalkyl compounds which exist predominantly in the intramolecularly hydrogen-bonded enol form.Condensation of the alkynylquinoxalines with diethyl sodiomalonate, and related compounds, yields pyrido<1,2-a>quinoxalin-4-one derivatives. 2-Alkynyl-3-chloroquinoxalines are intermediates for convenient syntheses of pyrrolo<2,3-b>quinoxalines.

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1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1- aryl-4-methyl-1,2,4-triazolo[4, 3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, 1H NMR, 13C NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.

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The present invention relates to novel compounds of formula (I): or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.

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Das Chlor im 3-Chlorchinoxalin-2-carbaldehyd (Ia) wird nucleophil substituiert.CH-acide-Verbindungen und N-Nucleophile reagieren an der Formylgruppe.Das Hydrazon und das Oxim von Ia werden unter Ringschlussreaktionen zu 1,2,3-Triazolo<1,5-a>chinoxalin und 3-Cyanochinoxalin-2(1H)-on (VIII) uebergefuehrt.Mit Thioglykolsaeureethylester entsteht aus Ia Thieno<2,3-b>chinoxalin-2-carbonsaeureethylester IX).Die Umsetzung von 2-Chlor-3-methylchinoxalin (IIa) mit nucleophilen Reagenzien wird durchgefuehrt.

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In this paper, we introduce a novel and convenient method for the transformation of heterocyclic amides into heteocyclic thioamides. A two-step approach was applied for this transformation: Firstly, we applied a chlorination of the heterocyclic amides to afford the corresponding chloroheterocycles. Secondly, the chloroherocycles and N-cyclohexyl dithiocarbamate cyclohexylammonium salt were heated in chloroform for 12 h at 61C to afford heteocyclic thioamides in excellent yields.

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The present invention provides a kind of ethylene glycol compounds and its preparation method, preparation method route is short, high yield, the operation is simple. Compound VIII and IX as preparing the invention ethylene glycol compounds of the intermediate, compound VIII and IX is prepared as intermediate of the ethylene glycol compounds, high yield, high purity, it is suitable for industrial production. (by machine translation)

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This Letter describes the synthesis and SAR of two mGluR4 positive allosteric modulator leads, 6 and 7. VU001171 (6) represents the most potent (EC50 = 650 nM), efficacious (141% Glu Max) and largest fold shift (36-fold) of any mGluR4 PAM reported to date. However, this work highlights the challenges in hit-to-lead for mGluR4 PAMs, with multiple confirmed HTS hits displaying little or no tractable SAR.

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[Figure not available: see fulltext.] Pyrazolylquinoxalines act as important intermediates for the production of novel derivatives with potential biological applications. The current review covers the synthesis of 2(3)-(pyrazol-1(3(5),4)-yl)quinoxalines published from 1978 until present.

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A tetrabutylammonium iodide (TBAI)-catalyzed method for synthesis of 2-sulfolmethyl quinolone has been developed. Using water as solvent, a wide range of 2-sulfolmethyl quinolones were obtained in high to excellent yield. In addition, water and TBAI could be reused for five times without significant decrease of the yield of the corresponding product.

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A new efficient procedure for the chlorination of hydroxyquinoxaline derivatives into the corresponding chlorides is described. It has been found that the use of 1-chlorobutane produces the highest yield, reduces the time of reaction and facilitates direct formation of crystals without any purification.

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