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Imidazoquinoline and imidazonaphthyridine compounds having a nitrogen-containing heterocyclyl substituent at the 5-, 6-, 7-, or 8-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

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Oxazolidine – Wikipedia,
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A new method of arylating N-H and O-H containing compounds at room temperature with phenylboronic acids and cupric acetate in the presence of a tertiary amine promoter is described. Substrates include phenols, amines, anilines, amides, imides, ureas, carbamates, and sulfonamides.

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Organic synthesis boasts a wide array of reactions involving either radical species or ionic intermediates. The combination of radical and polar species, however, has not been explored to a comparable extent. Herein we present the hydrative aminoxylation of ynamides, a reaction which can proceed by either a polar-radical crossover mechanism or through a rare cationic activation. Common to both processes is the versatility of the persistent radical TEMPO and its oxidised oxoammonium derivative TEMPO+. The unique mechanisms of these processes are elucidated experimentally and by in-depth DFT-calculations.

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Oxazolidine – Wikipedia,
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A series of new chiral N,N?-sulfonyl bisoxazolidin-2-ones were synthesized starting from 2-aminoalcohols, sulfuryl chloride, and diethyl carbonate. This method utilizes natural amino acids as a source of chirality for the preparation of oxazolidinones.

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In this paper, standard molar energies of combustion of 2-oxazolidinone and 3-acetyl-2-oxazolidinone are reported. The experimental values, obtained from static-bomb combustion calorimetry, are ?(1465.42 ± 0.52) kJ·mol?1 and ?(2350.86 ± 0.84) kJ·mol?1, respectively. Using these combustion energy values, the standard molar enthalpies of formation, in crystalline phase, for the aforesaid compounds were calculated. These values were also determined, and the corresponding values are ?(430.30 ± 0.96) kJ·mol?1 and ?(617.72 ± 1.58) kJ·mol?1, respectively. The standard molar enthalpies of sublimation at T = 298.15 K were experimentally obtained by using the well-known Knudsen effusion method. The obtained values are (84.20 ± 3.22) kJ·mol?1 and (82.36 ± 1.84) kJ·mol?1, respectively. From the above experimental results, the standard molar enthalpies of formation in gas-phase of the compounds were derived. The values are: ?(346.10 ± 3.36) kJ·mol?1 and ?(535.36 ± 2.43) kJ·mol?1, respectively. To support the consistency of the experimental results presented here, enthalpies of formation in gas-phase, using the G4 composite method, were carried out as well. Experimental results suggest that the formation of intermolecular hydrogen bonds between the nitrogen (at ring’s position 3, see Fig. 1) with the oxygen (at ring’s position 2, see Fig. 1) contributes to the values of temperature and enthalpy of fusion, enthalpy of sublimation, and enthalpy of formation in solid phase.

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The copper-catalyzed reaction of arylidenecyclopropanes (1) with 2-oxazolidinone (2) gave the corresponding homoallylic oxazolidinones (3) in good to high yields. For example, the reaction of diphenylmethylenecyclopropane (1a), {bis(p-tolyl)methylenecyclopropane (1b), and {bis(p-anisyl)methylene}-cyclopropane (1d) in the presence of 10 mol% of Cu(OTf)2 without solvent proceeded at 120C, giving the corresponding homoallylic oxazolidinones (3a, 3b, and 3d) in 89, 80, and 58% yields, respectively.

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The reaction of alkynyl carboxylic acids, glyoxylic acid derivatives, and amines in the presence of a copper catalyst afforded the corresponding propargyl amines in good yields. The alkynyl carboxylic acid of this coupling reaction shows similar reactivity to that of a terminal alkyne, and the reactivity of the glyoxylic acid is almost identical to that of an aldehyde. When 2-aminopyridine was employed as the amine source, imidazopyridine derivatives were formed in good yields.

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A facile approach to (E)-alpha-haloenamide moieties from ynamides using bromo- or iodotrimethylsilane is described. The simple protocol enables a regio- and stereospecific hydrohalogenation of the triple bond in gram-scale and provides a general entry for synthesis of novel enamide analogues.

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New antibiotics are desperately needed to combat the increasing number of antibiotic resistant strains of pathogenic microorganisms. Natural products remain the most propitious source of novel antibiotics. It is widely accepted that actinobacteria are prolific producers of natural bioactive compounds. We argue that the likelihood of discovering a new compound having a novel chemical structure can be increased with intensive efforts in isolating and screening rare genera of microorganisms. Screening rare actinomycetes and their previously underrepresented genera from unexplored environments in natural product screening collections is one way of achieving this. Rare actinomycetes are usually regarded as the actinomycete strains whose isolation frequency is much lower than that of the streptomycete strains isolated by conventional methods. The relevance of the rare actinomycetes in this regard can also be demonstrated by the fact that many of the successful antimicrobial agents currently available in the market are produced by them. This chapter focuses on the bioactive secondary metabolites from rare actinomycetes with emphasis on their structures, relevant biological activities, source organisms, covering over 150 structures of different bioactive compounds produced by them with 84 citations. Its aim is to give the reader a brief view of the bioactive compounds from the rare actinomycetes and we wish to update our understanding of the potential of the rare actinomycetes by focusing on their biodiscovery potential. The emphasis is placed on new compounds discovered from these microorganims with bioactive potential. Copyright

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The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.

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