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Substituted isoxazoles for the treatment of inflammation

A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (III) wherein R7 is selected from hydroxyl, lower alkyl, carboxyl, halo, lower carboxylalkyl, lower alkoxycarbonylalkyl, lower alkoxyalkyl, lower carboxyalkoxyalkyl, lower haloalkyl, lower haloalkylsulfonyloxy, lower hydroxyalkyl, lower aryl (hydroxylalkyl), lower carboxyaryloxyalkyl, lower alkoxycarbonylaryloxyalkyl, lower cycloalkyl, lower cycloalkylalkyl, and lower aralkyl; and wherein R8 is one or more radicals independently selected from hydrido, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; or a pharmaceutically-acceptable salt thereof.

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Highly Site Selective Formal [5+2] and [4+2] Annulations of Isoxazoles with Heterosubstituted Alkynes by Platinum Catalysis: Rapid Access to Functionalized 1,3-Oxazepines and 2,5-Dihydropyridines

Platinum-catalyzed formal [5+2] and [4+2] annulations of isoxazoles with heterosubstituted alkynes enabled the atom-economical synthesis of valuable 1,3-oxazepines and 2,5-dihydropyridines, respectively. Importantly, this Pt catalysis not only led to unique reactivity dramatically divergent from that observed under Au catalysis, but also proceeded via unprecedented alpha-imino platinum carbene intermediates.

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A cyclooxygenase -2 inhibitor handkerchief auspicious past cloth method for the preparation of (by machine translation)

The invention discloses a cyclooxygenase -2 inhibitor for the preparation of handkerchief auspicious past cloth, the method comprises the following steps: 1) the benzoic aidoxime and the 1 […] phenyl methylacetylene in three (the 2 […] phenylpyridin) gathers the iridium (III), the magnesium oxide and the presence of triethylamine, the reaction is conducted under conditions of illumination to the 5 […] methyl -3,4 the […] diphenyl isoxazole; 2) the step 1) of the 5 […] methyl -3,4 the diphenyl isoxazole with chlorosulfuric acid […] stirring reaction, after the reaction, methylene chloride extraction, dichloromethane is in directly adding ammonia water, separating the organic phase, washed, concentrated, recrystallized with ethanol to obtain cutting past cloth ; 3) steps 2) logging in of the presence of triethylamine in past cloth with propionic anhydride reaction to obtain handkerchief auspicious past cloth. handkerchief auspicious past cloth of the present invention method for the preparation of simple steps, high yield and after treatment is simple. (by machine translation)

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Isoxazole – Wikipedia,
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A process for synthesizing the sodium impurity handkerchief auspicious past cloth preparation method (by machine translation)

The present invention provides a process for synthesis of sodium handkerchief auspicious past cloth preparation method of the impurity; this method, in order to 5-methyl -3,4-diphenyl-isoxazole as raw materials through sulfonation reaction, esterification reaction to synthesize the target product 4 – (5-methyl-3-phenyl-isoxazolyl) ethyl benzosulfonate. The impurity is gene toxic impurities handkerchief auspicious past cloth sodium, the research on the synthesis method of the impurity to the impurity spectrum and research handkerchief auspicious past cloth sodiumhandkerchief auspicious past cloth sodium the quality control of the product. The structural formula of the impurities as the following formula: . (by machine translation)

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Transition-metal-catalyzed uninterrupted four-step sequence to access trisubstituted isoxazoles

We describe herein a novel uninterrupted four-step sequence to access trisubstituted isoxazoles from readily available propargylic alcohols using sequentially iron and palladium catalytic systems. The advantages of such a strategy are illustrated by the high overall yields and the time-saving procedure that are reported.

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Atom-economic generation of gold carbenes: Gold-catalyzed formal [3+2] cycloaddition between ynamides and isoxazoles

The generation of gold carbenes via the gold-catalyzed intermolecular reaction of nucleophiles containing relatively labile N-O or N-N bonds with alkynes has received considerable attention during recent years. However, this protocol is not atom-economic as the reaction produces a stoichiometric amount of pyridine or quinoline waste, the cleaved part of the N-O or N-N bonds. In this article, we disclose an unprecedented gold-catalyzed formal [3+2] cycloaddition between ynamides and isoxazoles, allowing rapid and practical access to a wide range of synthetically-useful 2-aminopyrroles. Most importantly, mechanistic studies and theoretical calculations revealed that this reaction presumably proceeds via an alpha-imino gold carbene pathway, thus providing a strategically novel, atom-economic route to the generation of gold carbenes. Other significant features of this approach include the use of readily-available starting materials, high flexibility, simple procedure, mild reaction conditions, and in particular, no need to exclude moisture or air (“open flask”).

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Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: Reversal cyclooxygenase-2 selectivity by sulfonamide group removal

3,4-Diarylisoxazole analogues of valdecoxib [4-(5-methyl-3-phenylisoxazol- 4-yl)-benzensulfonamide], a selective cyclooxygenase-2 (COX-2) inhibitor, were synthesized by 1,3-dipolar cycloaddition of arylnitrile oxides to the enolate ion of phenylacetone regioselectively prepared in situ with lithium diisopropylamide at 0 C. The corresponding 3-aryl-5-methyl-4-phenyl- isoxazoles were easily generated by a dehydration/aromatization reaction under basic conditions of 3-aryl-5-hydroxy-5-methyl-4-phenyl-2-isoxazolines and further transformed into their benzenesulfonamide derivatives. The biochemical COX-1/COX-2 selectivity was evaluated in vitro by using the human whole blood assays of COX isozyme activity. Three compounds not bearing the sulfonamide group present in valdecoxib were selective COX-1 inhibitors.

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Isothiazole derivatives, process for the preparation thereof, and pharmaceutical composition including the same

The present invention relates to an isothiazole derivative of the following formula 1 or nontoxic salt thereof: 1wherein, R1 is hydrogen, alkoxy group or halogen group; R2 is methyl or amino group. According to the present invention, isothiazole derivative or nontoxic salt thereof having antipyretic, analgesic and antiphlogistic activity and an improved side effect; process for the preparation thereof; and pharmaceutical composition including the same can be provided.

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Functionalized diarylisoxazoles inhibitors of ciclooxygenase

The present invention refers to isoxazole derivatives, in particular diarylisoxazole derivatives inhibitors of cyclooxygenase (COX), in particular cyclooxygenase-1 (COX-1), to their pharmaceutical compositions, the process for their preparation and their use for the chemoprevention and treatment of inflammatory syndromes and in the prevention and treatment of carcinomas, in particular intestinal, ovarian and cutaneous carcinomas, in the treatment of pain syndromes, in particular after surgery, and in the cardiovascular field as antithrombotics/vasoprotectives/cardioprotectives.

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37928-17-9, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 37928-17-9, molcular formula is C16H13NO, introducing its new discovery.

Intermediate handkerchief auspicious past cloth sodium 5 – methyl – 3, 4 – diphenyl isoxazole preparation method (by machine translation)

The invention relates to a handkerchief auspicious past cloth sodium intermediate 5 – methyl – 3, 4 – diphenyl isoxazole preparation method, the preparation method, the steps are as follows: step 1, phenyl propynyl ons starting material, first with a amine hydrochloride condensation generating Z configuration of 1 – phenyl – 1 – propynyl – 3 – methyl – oxime; step 2, Z configuration of 1 – phenyl – 1 – propynyl – 3 – methyl – oxime with chlorinated iodine link addition reaction 3 – phenyl – 4 – iodo – 5 – methylisoxazole; step 3, 3 – phenyl – 4 – iodo – 5 – methyl-isoxazole substituted with phenyl boronic acid generated by the reaction in the 5 – methyl – 3, 4 – diphenyl-isoxazole. (by machine translation)

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Isoxazole – Wikipedia,
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