- Preparing method of fosfomycin trometamol
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to a preparing method of fosfomycin trometamol. The method includes the following steps of firstly, addingfosfomycin diaminoglycol to methyl alcohol, dropwise adding acetic anhydride or propionic anhydride at a room temperature, and removing the methyl alcohol after a stirring reaction to obtain white solid; secondly, adding absolute ethyl alcohol to the obtained white solid, conducting cooling and filtering, conducting washing with ethyl alcohol, and conducting vacuum drying to obtain the fosfomycintrometamol. According to the preparing method, the acetic anhydride which is low in price and low in toxicity is adopted as the raw material, cost is low, three wastes are few, the environment protection pressure is small, the yield is high, operation is simple and convenient, and the method is suitable for industrial production; in the preparing method, no low-temperature ion exchange column isneeded, the fosfomycin diaminoglycol and acetic anhydride react at a room temperature, the reaction conditions are mild, and energy consumption is low.
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Paragraph 0025; 0026; 0027
(2019/04/26)
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- Preparation method of high-content fosfomycin tromethamine
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The invention provides a synthesis method of fosfomycin tromethamine. The synthesis method comprises the following steps: (1) preparing fosfomycin di(alpha-methylbenzylamine/tromethamine) salt from fosfomycin phenylethylamine salt and tromethamine; (2) generating a reaction between the fosfomycin di(alpha-methylbenzylamine/tromethamine) salt prepared in the last step and an alcoholic solution of methylsulfonic acid or p-toluenesulfonic acid, stirring the mixture, cooling the mixture for crystallization, and performing filtration to obtain a wet coarse product; (3) refining the coarse product to obtain a fine product, and performing vacuum drying to obtain a dried fine product. The method is easy to operate and mild in reaction condition; the purity and the yield of a product are at an extremely high level.
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Paragraph 0053; 0054; 0055; 0056; 0057; 0058-0082
(2019/01/08)
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- Method for conveniently preparing fosfomycin trometamol
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The invention discloses a synthesis method of fosfomycin trometamol. The method comprises the following steps: (1), taking fosfomycin phenylethylamine salt and tromethamine as raw material to preparefosfomycin bis (alpha-methylbenzylamine/tromethamine) salt, adding an alcoholic solution of methanesulfonic acid or para-toluenesulfonic acid in a stirring condition, stirring and performing cooling crystallization after dropwise adding is accomplished, and filtering to obtain a crude wet product; and (2), refining the crude product to obtain a refined product, and performing vacuum drying, so asto obtain a refined dried product. The method is simple to operate and mild in reaction condition, and ensures that both the product purity and the yield achieve high levels.
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Paragraph 0038; 0039; 0040; 0041; 0042; 0043; 0044-0077
(2019/01/08)
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- METHOD FOR PREPARING FOSFOMYCIN AMMONIUM SALT
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Disclosed in the present invention is a method for preparing fosfomycin ammonium salts, comprising the following steps of: in an organic solvent, reacting fosfomycin phenylethylamine with an isocyanate, an isothiocyanate, a ketene, a dimer of an isocyanate, a dimer of an isothiocyanate, or a dimer of a ketene, and tromethamine; or, in an organic solvent, reacting fosfomycin bis-tromethamine with an isocyanate, an isothiocyanate, a ketene, a dimer of an isocyanate, a dimer of an isothiocyanate, or a dimer of ketene. The preparation method of the present invention can be achieved by only a one-step reaction, does not require a low-temperature ion-exchange column, has a high yield, low costs, fewer three-wastes, mild reaction conditions, and low energy consumption, and is convenient to operate and suitable for industrialization.
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Paragraph 0029; 0031; 0033; 0035; 0037; 0039; 0041; 0043
(2015/03/18)
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- A process for the preparation of fosfomycin salts
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A process for the preparation of fosfomycin trometamol, which comprises the reaction between fosfomycin disodium salt and a tromethamine acid salt with a carboxylic acid in a substantially anhydrous alcoholic solvent.
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Page/Page column 2
(2008/06/13)
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