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New preparation method of pulveres fosfomycin tromethamine salt

A technology of monotromethamine salt and monotromethamine, which is applied in the field of synthesis of fosfomycin monotromethamine salt, can solve problems such as unexplained crystallization and recrystallization, complex overall process, etc., and achieve cost Low cost, improved product quality, and convenient recycling

Inactive Publication Date: 2010-12-29
HUBEI XUNDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Chinese patent CN1060657 uses fosfomycin calcium salt as a raw material. The conditions for crystallization and recrystallization are not specified in this patent, and fosfomycin calcium needs to be obtained from levofosfomycin dextrophenethylamine salt or fosfomycin dialkali metal salt It is obtained by reacting with calcium chloride, the overall process is still relatively complicated, and the recycling of calcium oxalate must also be considered

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment one: Tromethamine acid sulfate method

[0040] Step (1), preparation of levofomycin disodium saline solution

[0041] Add 0.2mol 30% liquid caustic soda, 50ml water and 100ml toluene to the reaction flask, stir and cool down to 5°C, add 0.1mol levofosfomycin dexphenethylamine salt, wait until all solids disappear, stir for 30 minutes below 15°C, Still layering. Take the water layer and go directly to the next step.

[0042] Step (2), prepare mixed salt

[0043] Add 0.1 mol tromethamine acid sulfate to the aqueous solution of fosfomycin dialkali metal salt (preparation method: add 0.1 mol tromethamine and 0.1 mol sulfuric acid to 50 ml of water), then concentrate and dehydrate to dryness at low temperature to obtain a mixed salt. The concentration temperature does not exceed 50°C.

[0044] Step (3), preparation fosfomycin monotromethamine salt

[0045] Add 250ml of methanol to the mixed salt obtained in the upward step, stir at 30-40°C for 1 hour, and fil...

Embodiment 2

[0046] Embodiment two: tromethamine acid phosphate method

[0047] Step (1), prepare levofomycin dipotassium saline solution

[0048] Add 0.2mol potassium hydroxide, 50ml water and 100ml methyl tert-butyl ether into the reaction bottle, stir and cool down to 5°C, add 0.1mol levofosfomycin dextrophenethylamine salt, wait until all solids disappear, below 15°C Stir for 30 minutes, rest and separate layers. Take the water layer and go directly to the next step.

[0049] Step (2), prepare mixed salt

[0050] Add 0.1mol tromethamine acid phosphate aqueous solution to fosfomycin dipotassium salt solution (preparation method: add 0.1mol tromethamine and 0.1mol phosphoric acid to 50ml water), then concentrate and dehydrate to dryness at low temperature to obtain mixed salt. The concentration temperature does not exceed 45°C.

[0051] Step (3), preparation fosfomycin monotromethamine salt

[0052] Add 250ml of methanol to the mixed salt obtained in the previous step, stir at 30-40...

Embodiment 3

[0053] Embodiment three: tromethamine acid hydrochloride method

[0054] Step (1), preparation of levofomycin disodium saline solution

[0055] Add 0.2mol 30% liquid caustic soda, 50ml water and 100ml dichloromethane into the reaction bottle, stir and cool down to 5°C, add 0.1mol levofosfomycin dexphenethylamine salt, wait until all solids disappear, stir for 30 minutes below 15°C Minutes, static layering. Take the water layer and go directly to the next step.

[0056] Step (2), prepare mixed salt

[0057] Add 0.1mol tromethamine acid hydrochloride aqueous solution to fosfomycin disodium salt solution (preparation method: take 50ml of 4.0mol / L hydrochloric acid, add 0.1mol tromethamine, dissolve to obtain), then concentrate at low temperature Dehydrate to dryness to obtain mixed salts. The concentration temperature does not exceed 50°C.

[0058] Step (3), preparation fosfomycin monotromethamine salt

[0059] Add 250ml of methanol to the mixed salt obtained in the upward ...

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PUM

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Abstract

The invention relates to a new preparation method of pulveres fosfomycin tromethamine salt, which is simple and convenient and has low cost. The preparation method comprises the following steps: taking laevo-fosfomycin dextro-phenylethylamine salt as a raw material, and alkalifying the raw material with an alkali metal hydroxide for removing the dextro-phenylethylamine salt to obtain laevo-fosfomycin di-alkali metal salt aqueous solution; adding tromethamine acid inorganic salt aqueous solution to the obtained di-alkali metal salt aqueous solution, dehydrating at low temperature, and carrying out metathesis base exchange in methanol to filter out alkali metal inorganic salt; and adding an organic solvent to methanol solution to separate out the pulveres fosfomycin tromethamine salt, filtering and drying to obtain the pulveres fosfomycin tromethamine salt.

Description

technical field [0001] The invention relates to a new synthesis method of fosfomycin monotromethamine salt. The invention provides a more convenient and low-cost method for synthesizing fosfomycin monotromethamine salt. Background technique [0002] Fosfomycin is a broad-spectrum antibiotic. It is sensitive to Staphylococcus, Escherichia coli, Neisseria meningitidis, Neisseria gonorrhoeae, Salmonella typhi, Serratia, Proteus, Pseudomonas aeruginosa, Shigella and Helicobacter pylori, and can inhibit the synthesis of bacterial cell walls. Fungicides in the breeding season have inhibitory effects on most Streptococcus, Pseudomonas aeruginosa, Proteus mirabilis, and some Klebsiella pneumoniae and indole-negative Proteus. Fosfomycin is suitable for infection and sepsis in urinary tract, respiratory tract, digestive tract, gynecology, skin soft tissue and other parts. Oral administration can treat intestinal infection, urinary tract infection, Serratia infection, Helicobacter p...

Claims

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Application Information

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IPC IPC(8): C07F9/655
Inventor 易章国
Owner HUBEI XUNDA PHARMA
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