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Base-metal catalysts capable of enabling the assembly of heteroatom-dense molecules by cross-coupling of primary heteroarylamines and (hetero)aryl chlorides, while sought-after given the ubiquity of unsymmetrical di(hetero)arylamino fragments in pharmacophores, are unknown. Herein, we disclose the new ?double cage? bisphosphine PAd2-DalPhos (L2). The derived air-stable NiII pre-catalyst C2 functions well at low loadings in challenging test C?N cross-couplings with established substrates, and facilitates the first Ni-catalyzed C?N cross-couplings of primary five- or six-membered ring heteroarylamines and activated (hetero)aryl chlorides, with synthetically useful scope that is competitive with Pd catalysis.

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Anomeric O-hetarylation of tetra-O-benzyl- and tetra-O-acetylglucose (1a, b) can be directly performed with electrondeficient heteroaromatic/heterocyclic systems 2-14, which contain imide halide moieties. The reactions were carried out in the presence of a base and led, through an exchange of the halide by the glucopyranosyloxy moiety, to the products 2a-14a, 7b-14b. Predominantly or exclusively beta-products were obtained. Systems bearing more than one imide halide moiety, such as cyanuric fluoride (15) or 5-chloro-2,4,6-trifluoropyrimidine (16), can be employed for successive anomeric O-hetarylations. Investigation of the glycosyl donor properties of O-glucosyl heteroaromatic imidates with 6-O-and 4-O-unprotected glucose derivatives 18 and 19 as acceptors and comparison of the results obtained with data for the corresponding beta-trichloroacetimidates 17abeta and 17bbeta, reveals that 2,3,5,6-tetrafluoropyridin-4-yl glucopyranosides 14abeta and 14bbeta exhibit similar properties. For specific tasks, for instance alpha-glucopyranoside formation, 14abeta may even be advantageous.

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Cavitands are synthetic receptors typically based on resorcin[4]arenes, macrocyclic concave compounds that are readily available and can be easily transformed into deeper synthetic cavities by attachment of aromatic spacers or panels. The use of aromatic heterocycles is ubiquitous in these structures, either for synthetic convenience, to regulate the dynamic and self-assembling properties of these receptors, or to provide suitable coordination environments for metal-functionalized receptors.

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2-(4,5-Dihydro-1H-imidazol-2-yl)thiophenol (1) and analogous compounds react with biselectrophiles under ring closure to give doubly (or more) annulated heterocyclic systems containing six- or seven-membered rings.

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The reaction of thiocarbohydrazide with carboxylic acids at the melting temperature allows an improved preparation of 5-substituted-4-amino-3-mercapto 1,2,4-triazoles 1a g. Compound 1a reacted with 2-bromopropionic acid to give acid derivative 2. The latter was reacted with a mixture of acetic anhydride and triethylamine to afford the mesoionic compound 3. Heating of compound 3 in ethanol gave the ester derivative 4, which on alkaline hydrolysis in methanol gave ketone derivative 5. Substituted 1,2,4-triazolo [3,4-b]-6H-1,3,4-thiadiazine 6h,i and 7 were synthesized by reaction of 1a with acetylacetone, ethyl acetoacetate and chloroacetamide. Heterocyclic systems 8 and 9 were prepared through the reaction of 1a with 2,3-dichloro-1,4-naphthoquinone and 2,3-dichloroquinoxaline. In addition, thenoyl isothiocyanate, thenoyl chloride, 2-thiophenecarbaldehyde, and p-chlorophenyl isocyanate reacted with compound 1a to afford 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole ring system 10, 11, and urea derivative 12. 1,2,4-Triazolo[3,4-b]-5H-pyrazole derivatives 14j,k were prepared through the reaction of compound 1a with 3-chloro-2,4-pentandione and ethyl-2-chloroacetoacetate. Compound 14j was treated with hydrazine to afford products 15, 16, and 17 depending on the type of hydrazine derivative and reaction conditions. Compound 19 was synthesized by refluxing of compound 14j with hydroxylamine hydrochloride to afford the corresponding oxime derivative 18 followed by treatment with thenoyl chloride.

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Several new derivatives of imidazo[1,2-a]quinoxalines have been synthesized in good to excellent yields starting from arylaminoisoxazol-5(2H)-ones and 2,3-dichloroquinoxaline through a rearrangement under mild base-catalyzed conditions.

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The present invention refers to organic electroluminescent compound quinoline or quinoline […] fusion pyrrole-cover derivatives and their relates to manufacturing method. Of the present invention method produced an organic electro luminescence display in a compound, whose driving voltage is low, current efficiency and power efficiency and luminous efficiency or the like such as, high purity a cancellous operating life an organic electro luminescence display in a may provide a. (by machine translation)

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Novel azine-helicene hybrids (pyridine-, pyrazine- and quinoxaline-fused along the central ring [5]helicenes) have been prepared in good overall yields through a five-step synthetic sequence. Commercially available 2,3-dihaloazines were used as starting materials. To discern the effect of merging an azine moiety within a helical skeleton, the X-ray structures, UV/Vis absorption spectra, cathodic and anodic electrochemistry of the helicene hybrids were investigated and compared to that of the parent [5]helicene.

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In this work, new derivatives of the 1,2,3-triazole-linked quinoxaline ring system are prepared by the reaction of 2-chloro-3-(prop-2-ynyloxy)quinoxaline or 2,3-bis(prop-2-ynyloxy)quinoxaline with aromatic azides via copper-catalyzed azide-alkyne cycloaddition reactions in the presence of the Schiff base ligands. These reaction procedures have the advantages of high-to-excellent yields, short reaction times, mild experimental conditions, and operational simplicity. The synthesized compounds were screened against the three bacterial strains Micrococcus luteus, Pseudomonas aeruginosa, and Bacillus subtilis. The anti-bacterial activity of 6b against P. aeruginosa was better than that for the standard drug (tetracycline).

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5,6-Di-(p-tolyl)imidazo<2,1-b>thiazol-3(2H)-one (IIIa), its 2-methyl analogue (IIIb), 7H-2,3-bis-(p-tolyl)imidazo<2,1-b><1,3>thiazin-5(6H)-one (V) and 3-substituted-5,6-di-(p-tolyl)imidazo<2,1-b>thiazoles (VII) have been synthesised in two steps; whereas 3-methyl-5,6-di-(p-tolyl)imidazo<2,1-b>thiazole hydrochloride (VIIe), 2,3-di-(p-tolyl)imidazo<2',1':2,3>thiazolo<4,5-b>quinaxoline (VIII) and 2,3-dihydro-5,6-di(p-tolyl)imidazo<2,1-b>thiazole hydrobromide (IX) are obtained in one step only starting from 2-mercapto-4,5-di-(p-tolyl)imidazole (I).

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