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The anion of 2-aryl acetonitrile derivatives reacted with a variety of heteroaryl chlorides or bromides in an SNAr manifold to afford intermediate anions which were susceptible to oxidation. The addition of sodium peroxide and aqueous NH4OAc solution effected oxidation to afford aryl heteroaryl ketones in good yields. Aryl acetonitrile derivatives are thus umpolung-type synthons of the corresponding aryl carbonyl functionality.

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Quinoxaline – Wikipedia,
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Focused microwave irradiation of a series of halogenated nitrogen heterocycles and different kinds of nucleophiles in the presence of a catalytic amount of indium trichloride leads to the efficient and completely regioselective generation of aromatic C-C and C-N bonds. The method is simple, rapid, general and inexpensive, and can be performed without the use of dried solvents. Most of the synthetized compounds are new and in many cases the work-up required only filtration. Furthermore, this is the first example of the use of a Lewis acid as a catalyst for heteroarylation, vinylation and amination reactions on pi-deficient heterocyclic substrates.

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Quinoxaline – Wikipedia,
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Different substituted pyridinium N-heteroarylaminides have been prepared in one step from N-aminopyridinium iodide and the corresponding heteroaryl halide by two alternative routes. The use of Pd catalysis allowed the easy preparation of products from the less reactive haloheterocycles. The use of water as a solvent in conjunction with microwave heating dramatically diminishes the reaction time without having an adverse effect on reaction yields.

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The synthesis of 2-(4-nitrophenoxy)quinoxaline (3) is described. The reaction of (3) with hydroxide ion was studied in the presence and absence of micellar systems. Cationic micelles of cetyltrimethylammonium chloride and bromide (CTACl and CTABr) and tetradecyltrimethylammonium chloride and bromide (MTACl and MTABr) speed the reaction of (3) with hydroxide ion. The second-order rate constants at the micellar pseudophase are smaller than the second-order rate constant in water.

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Novel 1,4-diazine-based dyes of the D?pi?A type, possessing triphenylamine as an electron-donating group, have been developed. Fluorescence studies have demonstrated that emission of these fluorophores is sensitive towards different nitroaromatic compounds and aliphatic amines, both in solutions and in a vapor phase. Moreover, these compounds can be considered as ?naked-eye? fluorescent probes for solution polarity because they possess pronounced solvatochromic properties. Therefore, these compounds have to be regarded as potential multifunctional chemosensors for monitoring hazardous organic substances.

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An efficient and mild protocol has been developed for the Minisci acylation reactions of nitrogen-containing heteroarenes with alpha-keto acids. Distinct from the conventional Minisci acylation conditions, the chemistry was performed using non-noble metal Fe(II), instead of expensive Ag(I) salt, as catalyst. A wide range of substrates, including aliphatic or aromatic alpha-keto acids, as well as various N-heteroarenes, proved to be compatible with the protocol. Scale-up experiment also demonstrates the practicality of the approach.

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The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.

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The synthesis and biological evaluation of a novel series of 2-aminoquinoline substituted piperidines and tropanes incorporating a homotropene moiety is herein described. The series exhibits potent antagonism of the CXCR3 receptor and superior physicochemical properties. Compound 24d was found to be orally bioavailable, and PK/PD studies suggested it as a suitable tool for studying the role of CXCR3 in models of disease.

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Reaction of 2-chloroquinoxaline (1) with O-potassio-3,3-dimethyl-2-butanone (2) in liquid NH3 affords 1-(quinoxalin-2-yl)-3,3-dimethyl-2-butanone (3) via a thermal SRN1 mechanism and 2-tert-butylfuro<2,3-b>quinoxaline (4) via a competing ionic, addition-substitution process.When the SRN1 component of this … scheme is inhibited by di-tert-butyl nitroxide, only furoquinoxaline 4 is produced.O-Potassio-2,4-dimethyl-3-pentanone (5) reacts in a similar fashion with 1 to give SRN1 products, 2-(quinoxalin-2-yl)-2,4-dimethyl-3-pentanone (6) and 2-isopropylquinoxaline (8), along with quinoxalino<3,4-b>-2,2,5,5-tetramethylcyclopentanone (7), which results from addition-substitution.Reaction of 1 with O-potassio-3-methyl-2,4-pentanedione (9) affords low yields of 2-(quinoxalin-2-yl)butanone (10) by a sluggish SRN1 pathway.Reactions of 4-chloroquinazoline (11a) and 4-chloro-2-phenylquinazoline (11b) with enolate 2 provide excellent yields of the respective 4-quinazolinyl ketones 12a,b via an apparent SNAr mechanism.

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The present disclosure relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present disclosure further provides novel compounds and compositions as well as their methods of preparation and use. The disclosed JAK3 inhibitors may be used in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.

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