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N-tert-Butoxycarbonylated 2-oxazolidinones and tetrahydro-2-oxazinones are smoothly cleaved to acyclic N-Boc-amino alcohols on treatment with catalytic amounts of cesium carbonate at room temperature.The versatility of the procedure is demonstrated in a facile cleavage of highly functionalized heterocycles without epimerization and beta-elimination.

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Carbon fiber reinforced polymer (CFRP) composites were fabricated using a novel intrinsically healable isocyanurate-oxazolidone (ISOX) thermosetting matrix. After multiple delamination events, repeatable strength recovery of the composites has been demonstrated with a first healing efficiency up to 85% after thermal treatment. The healing mechanism results from transformation of the isocyanurate with epoxide groups to yield new oxazolidone rings at the fracture surface. This novel ISOX polymer utilizes commercial diglycidyl ether of bisphenol F (DGEBF) and toluene diisocyanate to produce a high cross-link density thermoset with a glass transition temperature (Tg) up to 285 C, and 99.5% of the composite weight remains at 300 C. The strength and stiffness of the composites are comparable with an engineering grade polymer matrix composite typically used in aerospace applications and the thermal stability places the materials in the polybismaleimide performance region although with greater toughness. This polymer exhibits the highest Tg of any self-healing material reported and is composed of low cost reactants, which gives the polymer great potential to function as a major component of an advanced structural composite for extreme environments.

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In an attempt to molecularly design liver X receptor (LXR) beta-selective agonists, we discovered that the combination of the 2-oxochromene moiety (head) and the imidazoline-2,4-dione moiety (tail) plays an important role in the expression potency and selectivity toward LXRbeta. We synthesized a series of 2-oxochromene derivatives and identified 43 as a LXRbeta-selective agonist that increased the HDL-C level without significantly elevating the TG level and resulted in a decreased lipid-accumulation area in the aortic arch in a high-fat-and-cholesterol-fed Bio F1B hamster. In this manuscript, we report the design, synthesis and pharmacology of these 2-oxochromene derivatives.

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A panel of 96 metalloprotease inhibitors was assembled using “click chemistry” by reacting eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the bidentate compounds against representative metalloproteases provided discerning inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7. The relative ease and convenience of the strategy in constructing focused chemical libraries for rapid in situ screening of MMPs is thereby demonstrated.

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A convenient and versatile method was developed for aza-Michael addition using a substoichiometric amount of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). Various nitrogen nucleophiles were efficiently introduced to alpha,beta-unsaturated carbonyl compounds employing 0.5 equiv of DBU. Furthermore, other heteroatomic nucleophiles could also be introduced successfully under the same reaction conditions.

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N-(2-hydroxyethyl)succinimide was formed with 80percent yield in the reaction of 2-oxazolidinone with succinic anhydride at 210 deg C instead of polyesteramides obtained from N-substituted 2-oxazolidinones.The identification based on the crystal structure determination.

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Layered double hydroxide (LDH)-based nanocomposites, fabricated by interacting LDHs with organic anions, are an emerging and active area in healthcare, environmental remediation, catalysis, and storage. Ciprofloxacin, sulfanilamide, and oxazolidinone, which exhibit antibacterial activity, are successfully intercalated in Zn-Al LDHs through anion exchange method. Synthesis of the precursor was confirmed by X-ray diffraction (XRD), transmission electron microscopy (TEM). Intercalation was successfully evaluated from XRD data. It has been found that both the nature and position of aromatic ring substituents effect the value of the basal distance and the host-guest hydrogen bond network. Evidence on interactions of intercalated anions with the inorganic layer has been confirmed from Fourier transform infrared absorption spectroscopy. Morphology of composites was studied by field emission scanning electron microscopy, and thermal stability was studied by thermogravimetry and differential thermal analysis. The novel nanocomposites demonstrated antibacterial activity against both Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. The designed organic-inorganic fusions may offer a promising antimicrobial nanomaterial for varied applications.

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Disclosed are 3′-N-desmethyl-3′-N-substituted-6-O-methyl-11-deoxy-11, 12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.

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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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Epoxy resins frequently have to meet a flame retardancy grade which can be accomplished by incorporating brominated reactive compounds, like tetrabromobisphenol A (TBBA) cured by a number of hardeners. A few brominated epoxy resins (BERs) have been prepared by curing a mixture of diglycidyl ethers of bisphenol A (DGEBA)/diglycidyl ethers of tertabromobisphenol A (DGETBBA) and different hardeners: dicyandiamide (DICY), 4,4?-diaminodiphenyl sulphone (DDS) and polyethylene polyamine (PEPA). The use of different hardeners strongly affects the thermal degradation behaviour of the BER. The main volatile products of pyrolysis, characterized by Pyrolysis-Gas Chromatography-Mass Spectroscopy (PY-GC-MS) at 423 C were phenol, isopropyl- and isopropenylphenol, mono- and di-brominated phenols, bisphenol A, mono-, di-, tri- and tetra-brominated bisphenol A. No nitrogen containing volatile products or HBr were evolved whereas SO2 is formed from BER cured with DDS (BER-DDS) and bromoethylene from BER cured with PEPA (BER-PEPA). Differences of 30-60 C in thermal stability of epoxy network have been found, depending on the hardener. The experimental evidence suggests a cooperative action of bromine and nitrogen in chain scission of epoxy resins. In particular the ability of the hardener in fixing HBr, evolved from TBBA units, seems to depend on the basicity of the N atom of the hardener: the lower the basicity, the lower the scavenging effectiveness and consequently the higher the thermal stability.

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