Simple exploration of 2,3-Dichloroquinoxaline

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Hepatitis C macrodyclic homoserine protease inhibitor (by machine translation)

The present invention relates to novel macrocyclic compounds and methods of use thereof. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

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Archives for Chemistry Experiments of 5-Nitroquinoxaline

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PROCESSES FOR PREPARING INDOLES

Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent.

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Conformationally constrained ortho- Anilino diaryl ureas: Discovery of 1-(2-(1?-Neopentylspiro[indoline-3,4?-piperidine]-1-yl)phenyl) -3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist

Preclinical antithrombotic efficacy and bleeding models have demonstrated that P2Y1 antagonists are efficacious as antiplatelet agents and may offer a safety advantage over P2Y12 antagonists in terms of reduced bleeding liabilities. In this article, we describe the structural modification of the tert-butyl phenoxy portion of lead compound 1 and the subsequent discovery of a novel series of conformationally constrained ortho-anilino diaryl ureas. In particular, spiropiperidine indoline-substituted diaryl ureas are described as potent, orally bioavailable small-molecule P2Y1 antagonists with improved activity in functional assays and improved oral bioavailability in rats. Homology modeling and rat PK/PD studies on benchmark compound 3l will also be presented. Compound 3l was our first P2Y1 antagonist to demonstrate a robust oral antithrombotic effect with mild bleeding liability in the rat thrombosis and hemostasis models.

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A new application about Quinoxalin-6-amine

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Nucleophilic vinylic substitution (SNV) of activated alkoxymethylene derivatives with 6-aminoquinoxaline

Treatment of 6-aminoquinoxaline with beta,beta-diactivated alkoxymethylene derivatives gave the corresponding N-(quinoxalin-6-yl)enamines. A variant of the SNV reaction mechanism was proposed for substitution of the alkoxymethylene compounds, on the basis of the structures of the precursor enol ether and the vinylic substitution product and on computations. Wiley-VCH Verlag GmbH & Co. KGaA, 2005.

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Properties and Exciting Facts About 2213-63-0

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Design, Synthesis, and Characterization of Quinoxaline Derivatives as a Potent Antimicrobial Agent

A series of quinoxalinone derivatives were synthesized by the reaction of o-phenylenediamine with oxalic acid to yield 1, 4-dihydro quinoxaline-2, 3-dione (1) and then treated with thionyl chloride to yield 2, 3 dichloro quinoxaline (2). This was further reacted with hydrazine hydrate to produce 2, 3-dihydrazinyl quinoxaline (3). This was finally reacted with substituted aromatic aldehydes to produce 2,3-bis[2-(sustituted benzylidine) hydrazinyl] quinoxalines (4). These quinoxalinone derivatives were characterized by infrared spectroscopy and nuclear magnetic resonance spectroscopy and MASS spectral data. All the synthesized compounds were evaluated for their antimicrobial activity. The results of the antimicrobial study revealed that compounds 4c, 4d, and 4i were active and exhibited better inhibitory activities as compared to standard drug ciprofloxacin. The results were further checked with protein legend interaction by using docking studies, and all the compounds exhibited good docking scores between ?8.72 and ?11.29?kcal/mol against dihydrofolate reductase protein fragment from Staphylococcus aureus (PDB ID-4XE6). Among all compound, 4c has shown maximum docking score and found in agreement to in vitro studies.

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Discovery of 7467-91-6

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Efficient microwave-assisted Pd-catalyzed hydroxylation of aryl chlorides in the presence of carbonate

An efficient microwave-assisted, palladium-catalyzed hydroxylation of aryl chlorides in the presence of a weak base carbonate was developed, which rapidly converts aryl and heteroaryl chlorides to phenols, and can be used when the aryl chloride is functionalized with a ketone, aldehyde, ester, nitrile, or amide.

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Simple exploration of Quinoxaline-2,3(1H,4H)-dione

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2,3-Disubstituted pyrrolo[2,3-b]quinoxalines via aminopalladation- reductive elimination

2,3-Disubstituted pyrrolo[2,3-b]quinoxalines have been prepared in good to high yield through the reaction of 2-alkynyl-3-trifluoroacetamidoquinoxalines with aryl and vinyl halides or triflates in the presence of Pd(PPh 3)4 and K2CO3 in MeCN at 100C.

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The important role of 2-Chloro-3-methylquinoxaline

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Pyrazolo[4?,3?:5,6]pyrano[2,3-b]quinoxalin-4(1H)-one: Synthesis and characterization of a novel tetracyclic ring system

(Chemical Equation Presented) Derivatives of the hitherto unknown ring system, pyrazolo[4?,3?:5,6]pyrano[2,3-b]quinoxalin-4(1H)-one, are synthesized in one step from the corresponding 1-substuituted or 1,3-disubstituted 2-pyrazolin-5-ones and 3-chloroquinoxaline-2-carbonyl chloride using calcium hydroxide in boiling 1,4-dioxane. The parent system carrying no substituent in positions 1 and 3 is obtained upon treatment of the 1-PMB (p-methoxybenzyl) protected congener with trifluoroacetic acid. Detailed NMR spectroscopic investigations including unambiguous chemical shift assignments of all 1H, 13C, and 15N resonances of the obtained tetracycles are reported.

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Brief introduction of 1448-87-9

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Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

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Extracurricular laboratory:new discovery of 1448-87-9

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Preparation of derivatives of 1-(2-pyrimidinyl)piperazine as potential antianxiety, antidepressant, and antipsychotic agents

(Chemical Equation Presented) This paper describes the preparation of twenty-eight derivatives of 1-(2-pyrimidinyl)piperazine as potential antianxiety, antidepressant, and antipsychotic agents. In twenty-six of the preparations a chloro nitrogen heterocycle was caused to react with an excess of 1-(2-pyrimidinyl)piperazine in the absence of solvent. A specific example is given above.

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