- Pyrrole compound, a preparation method and uses thereof
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The invention relates to a pyrrole compound, a preparation method and uses thereof, particularly to 4-(4-(methylsulfonyl)phenyl-1-propyl-3-(p-tolyl)-1H-pyrrole-2-ol (represented by a formula C) or a pharmaceutically acceptable salt thereof, a preparation
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Paragraph 0052; 0053; 0054; 0055
(2019/04/26)
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- Imrecoxib purifying method
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The invention relates to an imrecoxib purifying method, which comprises: purifying an imrecoxib crude product by using a first solvent system. According to the present invention, the process is stableafter the method is subjected to scale-up; and with the
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Paragraph 0031
(2019/04/26)
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- Preparation method of imrecoxib
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The invention provides a preparation method of imrecoxib. The preparation method of the imrecoxib comprises the steps that alpha-n-propylamino-4-methyl sulfonate acetophenone (II) and 4-methyl phenylacetate (III) are used as main raw materials, amidation
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- Preparation method of imrecoxib and intermediate thereof
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The invention discloses a preparation method of imrecoxib and an intermediate thereof. the preparation methoc comprises the following steps: 1) carrying out an amidation reaction between 2-amino-1-p-methylsulfonyl acetophenone and p-methylphenylacetyl halide so as to obtain N-[2-oxo-2-(4-methylsulfonylphenyl)]ethyl-4-methyl phenylacetamide; 2) carrying out a condensation and cyclization reaction on N-[2-oxo-2-(4-methylsulfonylphenyl)]ethyl-4-methyl phenylacetamide so as to obtain 3-p-methyl phenyl-4-p-methylsulfonylphenyl-3-pyrrolidine-2-ketone; and 3) carrying out a substitution reaction between 3-p-methyl phenyl-4-p-methylsulfonylphenyl-3-pyrrolidine-2-ketone and 1-halopropane or hydrocarbon sulfoacid propyl ester derivative so as to obtain imrecoxib; and preparing the intermediate of imrecoxib: N-[2-oxo-2-(4-methylsulfonylphenyl)]ethyl-4-methyl phenylacetamide or 3-p-methylphenyl-4-p-methylsulfonylphenyl-3-pyrrolidine-2-ketone. The reaction process is optimized by the synthetic route. Separation in each step is simpler, purity is higher, and ideal yield of the product also can be achieved.
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- Synthetic method of imrecoxib
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The invention discloses a synthetic method of imrecoxib. The synthetic method comprises the following steps: allowing (E)-1-p-methanesulfonylphenyl-1-nitro-2-p-tolylethylene and ethyl isocyanoacetateto undergo a condensation and cyclization reaction in a system containing an alkali reagent and a solvent; allowing the obtained 3-p-methylphenyl-4-p-methylsulfonylphenylpyrrole-2-carboxylate to undergo a reducing reaction at -78 DEG C in a system containing a reducing reagent and a solvent; allowing the obtained 3-p-methylphenyl-4-p-methylsulfonylphenylpyrrole-2-carbaldehyde to undergo an oxidation reaction in a system containing a hydrogen peroxide solution and a solvent; and allowing the obtained 3-p-methylphenyl-4-p-methylsulfonylphenyl-3-pyrrolidin-2-one and 1-halopropane or a hydrocarbonpropyl sulfonate derivative to undergo a substitution reaction in a system containing an alkali reagent and a solvent to obtain the imrecoxib. The synthetic method of the imrecoxib has the beneficialeffects that the reaction steps are simplified and optimized and the process is simple in operation, thereby being helpful to reduce cost; reaction impurities are less and controllable, so greennessand environment-friendliness are embodied; and initial raw materials and the used reagents are easily available.
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- A airuiairui past cloth intermediate and airuiairui past cloth preparation method (by machine translation)
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The invention discloses a airuiairui past cloth intermediate and airuiairui past cloth of the preparation method, comprising: in the presence of organic base, in an organic solvent with methyl acetic acid to make the α, α - two bromos - 4 - methylsulfonyl
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Paragraph 0059-0062; 0063-0065
(2018/12/14)
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- Synthesis method of airuiairui past cloth
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A synthesis method of airuiairui past cloth, which belongs to the pharmaceutical technical field of chemical synthesis. Steps: synthesis of 2 - n-propyl amino - 1 - to a sulfonyl acetophenone: will be N - n-propyl - β - hydroxy - 4 - methylsulfonyl-phenethylamine by oxidation reagent, solvent and water of the oxidation reaction in the system, to obtain the 2 - propyl amino - 1 - to a sulfonyl acetophenone; synthetic airuiairui past cloth: will be of 2 - n-propyl amino - 1 - to a sulfonyl acetophenone with methylphenyl acetate in the alkali reagent and solvent in the system of the condensation cyclization reaction, get airuiairui past cloth. Significantly simplify and optimize the reaction steps and the process is simple in operation, contributes to reducing the cost; the reaction less impurities, controllable, non-pollutants, reflected green environmental protection effect; the starting material and used easily obtained reagent, can be a large number of production to meet the use requirements of the raw material and is suitable for industrial production.
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Paragraph 0030; 0033-0034; 0040; 0043-0044
(2019/01/08)
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- Preparation methods of imrecoxib intermediate and imrecoxib
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The invention discloses preparation methods of an imrecoxib intermediate and imrecoxib. The preparation method of N-propyl-N-[2-oxo-2-(4-mesylphenyl)]ethyl-4-methyl phenyl acetamide as the imrecoxib intermediate comprises the following steps of performing substitution reaction on 2-amino-1-p-methylsulfonyl acetophenone and 1-halopropane in a system of an acid binding agent and a solvent to obtain2-propylamino-1-p-methylsulfonyl acetophenone; and enabling 2-propylamino-1-p-methylsulfonyl acetophenone and p-methyl phenylacetyl halide to perform amidation in the system of the acid binding agentand the solvent to obtain N-propyl-N-[2-oxo-2-(4-mesylphenyl)] ethyl-4-methyl phenyl acetamide. The preparation method of the imrecoxib comprises the following step of performing condensation and cyclization reaction on N-propyl-N-[2-oxo-2-(4-mesylphenyl)] ethyl-4-methyl phenyl acetamide in a system of an alkaline matter and a solvent on the basis. The synthetic route provided by the invention enables the reaction process to be more simple and post-treatment separation to be easier and is capable of acquiring ideal yield.
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- Preparation method of imrecoxib, and preparation method of imrecoxib intermediate
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The invention relates to a preparation method of imrecoxib, and a preparation method of an imrecoxib intermediate. The preparation method of the imrecoxib intermediate remarkably improves the yield ofthe intermediate (III). The preparation method of the imrecoxib is characterized in that p-methylsulfonylstyrene oxide used as an initial raw material undergoes nucleophilic ring opening, acylation,oxidation and cyclization to obtain the final product N-n-propyl-3-(4-methylphenyl)-4-(4-methylsulfonylphenyl)-2,5-dihydropyrrol-2-one. The method has the advantages of short route, simplicity in operation, and suitableness for industrial amplified production.
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Paragraph 0017; 0024; 0039; 0052; 0053
(2018/04/02)
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- A method for synthesizing [...]
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The invention discloses a synthesis method of imrecoxib and belongs to the field of drug synthesis. The method comprises the following steps: reacting p-toluene acetyl halide with propylamine to produce a compound III p-toluene levulinic amine; reacting the compound III with p-methylsulfonyl chloroacetophenone under an alkaline condition to produce a compound V; and then cyclizing to obtain a compound VII, namely n-propyl-3-(4-methyl phenyl)-4-(4-methylsulfonyl phenyl)-2,5-dihydro-1H-2-pyrrolidone. The method disclosed by the invention comprises simple reaction steps and can be put into industrial production easily.
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- Sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones, preparation method, and medical use thereof
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The invention relates to sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones compounds having formula (I) wherein R1 is selected from the group consisting of 4-methylsulfonyl, 4-aminosulfonyl, hydrogen, 2-, 3-, or 4-halogen, C1-C6
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Page/Page column 16-17
(2008/06/13)
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