- A process for the preparation of sodium compound handkerchief auspicious past cloth and wherein the intermediate impurity, preparation method and application
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The invention provides parecoxib sodium which is prepared by controlling an intermediate impurity and in particular provides a preparation method of a parecoxib sodium compound as well as the intermediate impurity and an application of the parecoxib sodium compound. According to the preparation method provided by the invention, 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol is used as an isomer impurity for preparing 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an intermediate of the parecoxib sodium, the quality of the 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol is controlled in the preparation of the parecoxib sodium, specifically, the impurity content is required not to be higher than 0.5 percent, and an important significance is provided for the product quality of the parecoxib sodium; by obtaining the 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an isomer impurity of the important 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol and further studying 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol in the aspects of preparation process, detection process and purification process, important quality monitoring significance is provided for the process with the 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an industrial production raw material.
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- Method for preparing parecoxib for treating postoperative pain
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The invention discloses a method for preparing parecoxib for treating postoperative pain. The method comprises the following steps: 1) conducting a contact reaction between 3,4-diphenyl-4-(1-pyrrolidyl)-3-butene-2-one and ammonium acetate in acetic acid; after the reaction, diluting dichloromethane; regulating the pH value to 6-7 with saturated sodium bicarbonate; concentrating the organic phase and washing; recrystallizing with ethanol; and drying to obtain 5-methyl-3,4-diphenyl isoxazole; 2) stirring the obtained 5-methyl-3,4-diphenyl isoxazole and chlorosulfonic acid for reacting; adding anion exchange resin, and dropwise adding saturated ammonium chloride and dichloromethane for extraction; washing and concentrating; and recrystallizing with ethanol to obtain valdecoxib; and 3) enabling the valdecoxib obtained in the step 2) to react with propionic anhydride in the presence of triethylamine to obtain parecoxib. The method for preparing parecoxib, disclosed by the invention, has the advantages of simple steps, mild conditions and high yield.
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Paragraph 0005; 0059; 0060; 0061
(2017/01/12)
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- METHOD FOR THE PREVENTION OR TREATMENT OF PAIN, INFLAMMATION, AND INFLAMMATION-RELATED DISORDERS WITH A COX-2 SELECTIVE INHIBITOR IN COMBINATION WITH A NITRIC OXIDE-DONATING AGENT AND COMPOSITIONS THEREWITH
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Methods and compositions are described for the prevention or treatment of pain, inflammation, and inflammation-related disorders in a subject in need of such prevention or treatment, the method comprising administering to the subject a cyclooxygenase-2 selective inhibitor in combination with a nitric oxide-donating agent. Also described are therapeutic and pharmaceutical compositions and kits that are useful in the present invention.
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Page/Page column 73-74
(2008/06/13)
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- METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES
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The disclosure provides a method for the preparation of a diarylisoxazolé sulfonamide compound comprising contacting a deoxybenzoin with a secondary amine to form a diarylenamine compound; contacting the diarylenamine compound with an acetylating agent to form an acetyl diarylenamine compound; contacting the acetyl diarylenamine compound with a source of hydroxylamine to form an diaryl isoxazolol compound; eliminating water from the diaryl isoxazolol compound to form a diaryl isoxazole compound, chlorosulfonating the diarylisoxazole compound to form a chlorosulfonyl diaryl isoxazole compound; and contacting the chlorosulfonyl diaryl isoxazole compound with a source of ammonia to form the diarylisoxazole sulfonamide compound.
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Page/Page column 28-30; 34-35
(2008/06/13)
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- Method for preparing benzenesulfonyl compounds
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The present disclosure provides a method for the preparation of aromatic sulfonyl halides by contacting a substituted phenyl compound with a halosulfonic acid and trifluoroacetic acid. The present disclosure further provides a method for the preparation of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide which is useful in treating cyclooxygenase-2 related disorders.
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- Crystalline parecoxib sodium
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Parecoxib sodium is provided in a crystalline form that is substantially anhydrous and substantially nonsolvated. Various such anhydrous, nonsolvated crystal forms have been identified, including Forms A, B and E as described herein. Also provided is a parecoxib sodium drug substance wherein at least about 90% of the parecoxib sodium is in one or more anhydrous, nonsolvated crystal forms. Such a drug substance is a storage-stable intermediate that can be further processed, for example by dissolution or slurrying in an aqueous medium together with one or more parenterally acceptable excipients, followed by lyophilization of the resulting solution or slurry to provide a reconstitutable injectable composition suitable for therapeutic use.
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- Substituted isoxazoles for the treatment of inflammation
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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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- Isoxazole compounds as cyclooxygenase inhibitors
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A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I STR1 wherein R1, R2, and R3, are described in the specification.
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