Fosfomycin disodium preparation method

A technology of fosfomycin sodium and sodium hydroxide, which is applied in chemical instruments and methods, compounds of group 5/15 elements of the periodic table, organic chemistry, etc., and can solve the problem of large loss of anhydrous ethanol, non-recyclable application, and spray drying Problems such as huge equipment, to achieve the effect of reducing production costs and reducing consumption

Inactive Publication Date: 2019-04-30
HUBEI XUNDA PHARMA
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  • Claims
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Problems solved by technology

The sodium methoxide method is to dissolve with methanol and use acetone for crystallization. This method uses a mixed solvent, which makes solvent separation difficult and cannot be recycled. The sodium hydroxide aqueous solution method needs to use a large amount of dehydrated alcohol so

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  • Fosfomycin disodium preparation method
  • Fosfomycin disodium preparation method

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Embodiment 1

[0017] The preparation process of fosfomycin sodium is as follows:

[0018] a. Sodium hydroxide is dissolved in industrial ethanol, and the temperature is lowered for subsequent use;

[0019] b. Put the solid left phosphorus and right amine salt and industrial ethanol into the reaction kettle, control the temperature at 30-35°C, add dropwise the sodium hydroxide ethanol solution dissolved in the above step a until the left phosphorus and right amine in the reaction kettle All the salt solids are dissolved, stop dripping, add activated carbon for decolorization, then filter and discard the filter residue to retain the filtrate;

[0020] c. Continue to slowly add sodium hydroxide ethanol solution dropwise to the filtrate obtained in the above step b until the pH value of the solution reaches 10.5, stop the dropwise addition, stir and crystallize after 10h and centrifuge to obtain a large amount of white solid crystals;

[0021] d. Put the white solid crystals obtained in the ab...

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Abstract

The invention discloses a fosfomycin disodium preparation method. According to the method, based on the high solubility of fosfomycin monosodium in industrial ethanol and the almost insolubility of fosfomycin disodium in industrial ethanol, industrial ethanol is used as the single solvent, and sodium hydroxide reacts with L-cis-1,2-epoxypropylphosphonic acid-D-alpha-phenylethylamine in industrialethanol, wherein fosfomycin disodium can be formed to cause turbidity when the added sodium hydroxide is excessive so as to accurately control the adding amount of sodium hydroxide based on the condition, such that the adding of sodium hydroxide is stopped before the formation of fosfomycin disodium; then active carbon is added to decolorize, and impurities are removed to obtain the mixed solutionof impurity-free fosfomycin monosodium and industrial ethanol; and a sodium hydroxide ethanol solution is added to the mixed solution of impurity-free fosfomycin monosodium and industrial ethanol, and a reaction is performed to obtain the final product fosfomycin disodium, wherein no impurity exist, and the filtrates in the steps c and d can be continuously and repeatedly used after centrifugal filtration, such that the consumption of the solvent ethanol is substantially reduced, and the production cost is reduced.

Description

technical field [0001] The invention relates to the field of organic synthesis, in particular to a preparation method of fosfomycin sodium. Background technique [0002] As a new type of antibiotic drug, fosfomycin sodium usually exists in the form of sodium salt, calcium salt and ammonium salt, among which sodium salt is used for intravenous drip or injection, and its antibacterial spectrum is wider than that of penicillins and cephalosporins. Widely used in Japan and Europe. [0003] There are many preparation methods for fosfomycin sodium, such as sodium methoxide method, sodium hydroxide solution method and spray drying method. The sodium methoxide method is to dissolve with methanol and use acetone to crystallize. This method uses a mixed solvent, which makes solvent separation difficult and cannot be recycled. The loss of water ethanol is relatively large. Spray-drying is to directly obtain fosfomycin sodium salt by spraying the sodium salt aqueous solution with spr...

Claims

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Application Information

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IPC IPC(8): C07F9/655
CPCC07F9/65502C07F9/65505
Inventor 张钜寿吴刚江海洋许广益李亮王运发马路军
Owner HUBEI XUNDA PHARMA
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