- Preparation method of thioether
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The preparation method comprises the following steps: (a) reacting a halogenated alkyl pyridine derivative or a salt thereof with 2 -mercaptobenzimidazole derivative in a water-soluble organic solvent under basic conditions. (b) The reaction solution obtained in step (a) was subjected to first devitrification step and second devitrification step, and purified. The prepared thioether is low in water content, uniform in water content and high in thioether purity, facilitates control of the water content of a reaction system in a subsequent thioether asymmetric oxidation reaction, and ensures high selectivity and reproducibility of asymmetric oxidation reaction. In addition, the preparation method of the thioether provided by the invention is simple in process and good in repeatability, and is more conducive to large-scale production.
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Paragraph 0050-0055; 0060-0066
(2021/11/03)
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- Pharmaceutical composition containing ilaprazole sodium and preparation method thereof
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The invention relates to a pharmaceutical composition containing ilaprazole sodium and a preparation method thereof. The pharmaceutical composition is prepared from the ilaprazole sodium and ilaprazole derivatives, wherein the ilaprazole derivatives comprise ilaprazole sulfone, ilaprazole thioether, ilaprazole carboxyl ylide, ilaprazole hydroxyl ylide, ilaprazole mercaptomethyl ylide, ilaprazole methyl ylide, ilaprazole thiocyanmethyl ylide, ilaprazole dithiodimer, ilaprazole trithiodimer and ilaprazole nitrogen oxide. The pharmaceutical composition can be used for treating peptic ulcer hemorrhage and stress ulcer, and preventing upper gastrointestinal hemorrhage caused by serious illnesses.
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Paragraph 0032-0034
(2019/01/14)
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- Method for synthesizing intermediate of Ilaprazole sodium salt
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The invention provides a method for synthesizing an intermediate of an Ilaprazole sodium salt. The method comprises the following steps: (1) adding a starting raw material, i.e., 5-(1H-pyrrol-1-yl)-2-mercaptobenzimidazole into a reaction bottle containing a sodium hydroxide solution and deionized water, and carrying out stirring with heating; and (2) adding a mixture solution of 2-chloromethoxy-4-methoxy-3-methylpyridine hydrochloride and deionized water into the reaction bottle, and carrying out a reaction until the reaction ends, thereby obtaining 5-(1H-pyrrol-1-yl)-2-[(4-methoxy-3-methyl-2-pyridyl)-methylthio]-1-H-benzimidazole. According to the method, the yield reaches 86% and is far higher than that of the existing technologies, and the used solvent is environmentally friendly and is pollution-free to environment; and the reaction operation is simple, the reaction conditions are easily controlled, and the obtained product is high in purity.
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Paragraph 0017-0042
(2017/10/26)
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- SUBSTITUTED SULFOXIDE COMPOUNDS, METHODS FOR PREPARING THE SAME AND USE THEREOF
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Disclosed are an optically pure compound having formula (I), its pharmaceutically acceptable salt and its pharmaceutically acceptable solvate, and a use thereof in manufacturing medicaments and pharmaceutical compositions. A process for preparing the compound defined therein is also provided. Formula (I).
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Page/Page column 6; 13; 16-17
(2008/06/13)
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- Substituted sulfoxide compounds, methods for preparing the same and use thereof
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Disclosed are an optically pure compound having formula I, its pharmaceutically acceptable salt and its pharmaceutically acceptable solvate, and a use thereof in manufacturing medicaments and pharmaceutical compositions. A process for preparing the compound defined therein is also provided.
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Page/Page column 3; 6; 7
(2008/06/13)
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