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DERIVATIVES OF 2-[2-(BENZO- OR PYRIDO-) THIAZOLYLAMINO]-6-AMINOPYRIDINE, USEFUL IN THE TREATMENT OF RESPIRATORIC, ALLERGIC OR INFLAMMATORY DISEASES

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity

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The Dichotomy of Gold-catalyzed Interplay between Cyanamides and Ynamides: Controllable Switch from [2+2+2] to [4+2] Cycloaddition

The gold-catalyzed interplay between cyanamides and ynamides demonstrates condition-dependent mechanistic dichotomy. [2+2+2] Cycloaddition proceeds under kinetically controlled conditions to give 2,4,6-triaminopyrimidines (19 examples, up to 99%). Under thermodynamically controlled conditions, the reactivity switches from [2+2+2]- to [4+2] cycloaddition; the latter [4+2] reaction accomplishes 1,3-diaminoisoquinolines (19 examples, up to 97%). The advantages of both methods include regioselectivity, mild reaction conditions (even for the thermodynamically controlled [4+2] reaction) and the possibility of introducing a variety of dialkyl, diaryl, and heterocyclic amino substituents into the target pyrimidine and isoquinoline cores. The reactions were conducted on gram scales and the versatility of the obtained products was demonstrated by post-functionalizations. (Figure presented.).

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2-(1-HETEROARYLPIPERAZIN-4-YL)METHYL-1,4-BENZODIOXANE DERIVATIVES AS ALPHA2C ANTAGONISTS

Compounds of formula I (formula I), wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2 or 3 N, O or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

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Highly efficient KF/Al2O3-catalyzed versatile hetero-Michael addition of nitrogen, oxygen, and sulfur nucleophiles to alpha,beta-ethylenic compounds

The first example of KF/Al2O3-catalyzed versatile hetero-Michael addition reaction of nitrogen, oxygen, and sulfur nucleophiles was developed for facile preparation of organic compounds of widely different structures. In contrast with the existing methods using many acidic catalysts, this method is very general, simple, high-yielding, environmentally friendly, and oxygen and moisture tolerant.

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Visible-Light-Mediated Liberation and In Situ Conversion of Fluorophosgene

The first example for the photocatalytic generation of a highly electrophilic intermediate that is not based on radical reactivity is reported. The single-electron reduction of bench-stable and commercially available 4-(trifluoromethoxy)benzonitrile by an organic photosensitizer leads to its fragmentation into fluorophosgene and benzonitrile. The in situ generated fluorophosgene was used for the preparation of carbonates, carbamates, and urea derivatives in moderate to excellent yields via an intramolecular cyclization reaction. Transient spectroscopic investigations suggest the formation of a catalyst charge-transfer complex-dimer as the catalytic active species. Fluorophosgene as a highly reactive intermediate, was indirectly detected via its next downstream carbonyl fluoride intermediate by NMR. Furthermore, detailed NMR analyses provided a comprehensive reaction mechanism including a water dependent off-cycle equilibrium.

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Synthesis of some 2-Oxazolidinones in mild conditions

One step efficient protocol for the synthesis of 2-oxazolidinones in paste chemical medium is described under microwave activation with 80 % yield.

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Nanocatalysts for chemical transformation of carbon dioxide

This review deals with the applications of nanocatalysts in chemical transformation of CO2, a field that has attracted great interest in the chemical, fuels, materials, and industrial communities. Literature has been surveyed from 2010 to 2017.

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Modification of epoxy resin: A comparison of different types of elastomer

Composites were prepared using epoxy resin (ER), carboxyl-terminated butadiene acrylonitrile copolymer (CTBN) and hydroxyl-terminated polybutadiene (HTPB), in different proportions. A chemical link between the HTPB and the epoxy resin was promoted employing tolylene diisocyanate (TDI). The reactions between elastomers and epoxy resin were followed by FTIR. The mechanical properties of the composites were evaluated and the microstructure was investigated through scanning electronic microscopy (SEM). The results showed that the impact resistance of CTBN-modified ER was superior to that of the pure epoxy resin. For the composites with HTPB, the impact resistance increased with elastomer concentration up to three parts per hundred parts of resin (phr). Higher concentrations of HTPB resulted in larger particles and gave lower impact values.

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Nickel-catalyzed reductive and borylative cleavage of aromatic carbon-nitrogen bonds in N-aryl amides and carbamates

The nickel-catalyzed reaction of N-aryl amides with hydroborane or diboron reagents resulted in the formation of the corresponding reduction or borylation products, respectively. Mechanistic studies revealed that these reactions proceeded via the activation of the C(aryl)-N bonds of simple, electronically neutral substrates and did not require the presence of an ortho directing group.

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METHOD FOR PRODUCING 1,4-DIPHENYL AZETIDINONE DERIVATIVES

The invention relates to a method for producing 1,4-diphenyl azetidinone derivatives from suitably protected beta-substituted amino amides, in the presence of silylation agents. Said method uses cyclization catalysts that comprise phosphonium ions as the cation of formula (XII), and ions of the following general formulas (a), (b), (c) or (d) as the anion. In said formulas, the symbols, substituents and indices are defined as follows: Z = C=O, C=S, S=O, SO2 or C=NR20; K = O, S, NR21 or CR22R23; L = NR24 or CR25R26; n = 0 or 1; M = O, C=O, NR27 or CR28R29; Q = O, S, NR30, CR31R32,C=O, C=S, S=O, SO2 or C=NR34; R = CR35 or N; T = CR36 or N; U = CR37 or N; V = CR38 or N; the groups R16 to R19can represent, for example, aryl or (C1-C15) alkyl, aryl(C1-C10)alkene, and the groups R20 to R32 and R34 to R38 can represent in addition H or heteroaryl; R39 and R40 represent, for example (C1-C6) alkyl. The anion can also be R41O,R42COOor Cl, Br or I (combined with Ag2O).

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