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Novel method for preparing fosfomycin phenylethylamine

A technology of levophosphorus amine salt and a new method, which is applied in the field of preparing fosfomycin levophosphoryl amine salt, and can solve the problems of wasting time, fewer reaction steps, and increased cost

Active Publication Date: 2013-05-22
JIANGSU SKYRUN PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Disadvantages: In the splitting process, it is necessary to repeat dozens of times of crystallization to obtain the left phosphorus and right amine salts. First, it is a waste of time. Second, the overall split rate is not high, and the cost increases
At the same time, the invalid compound dexaphosphorus and leftammonium salt accounted for half of the composition, which caused a waste of resources if it was not utilized.
[0012] The present invention aims at above-mentioned present situation, provides a kind of raw material cheap and easy to obtain, toxicity is little, reaction step is few, and side reaction is few, and three wastes are few, this splitting method that is suitable for industrialized large-scale production, and this method is to use water as main solvent, Add appropriate amount of DMSO to avoid contamination in traditional resolution methods

Method used

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  • Novel method for preparing fosfomycin phenylethylamine
  • Novel method for preparing fosfomycin phenylethylamine

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Embodiment Construction

[0019] Set forth the present invention with example below:

[0020] 1. Synthesis of compound 1:

[0021] Take 1.2g (10mmol) cis-acrylophosphoric acid and absolute ethanol (5ml) into a 50ml three-necked bottle, stir to dissolve completely. Add dropwise from 0.5g Na 2 WO 4 Dissolve 0.13g EDTA-2Na in 5ml of water, then add 1.7g (15mmol) of 30% hydrogen peroxide, heat to 40 degrees to completely dissolve, and react for 1h. The reaction was monitored by high performance liquid chromatography. The insoluble matter was filtered off by cooling, and after the ethanol was distilled off, ethyl acetate was added to extract the generated DS fosfomycin, dried over anhydrous sodium sulfate, filtered, and concentrated to obtain a colorless oil (1.3 g, yield 94%).

[0022] 2. Dynamic split

[0023] Add 8 milliliters of deionized water and 2 milliliters of dimethyl sulfoxide into the reaction flask, start stirring, put 1.3 g of the product of the previous step fosfomycin into it, raise the...

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Abstract

The invention discloses a novel method for preparing fosfomycin phenylethylamine, which comprises the following steps: by using cis-propenylphosphonic acid as a raw material, carrying out oxidation and cyclization under the actions of a catalyst and an oxidizer, carrying out dynamic resolution under specific solvent conditions to precipitate levo-fosfomycin, adding a certain amount of dextro-phenylethylamine, reacting, and refining to obtain the levo-fosfomycin dextro-phenylethylamine. The preparation method has the advantages of low reaction cost, fewer steps, fewer byproducts and low environmental pollution, and is suitable for industrial mass production and prepration.

Description

technical field [0001] The invention relates to a new method for preparing fosfomycin left phosphorus and right ammonium salt. The invention provides a more convenient and low-cost synthesis method and belongs to the field of chemical synthesis. Background technique [0002] Fosfomycin is a broad-spectrum, low-toxic, non-sensitizing, non-resistance-resistant antibiotic that has a synergistic effect with most antibiotics. It is effective against Staphylococcus, E. , Serratia, Proteus, Pseudomonas aeruginosa, Shigella and Helicobacter pylori are all sensitive and can inhibit the synthesis of bacterial cell walls. Proteus, some Klebsiella pneumoniae and indole-negative proteobacteria have inhibitory effect. 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 pylori infectio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/655C07C211/27C07C209/68
Inventor 燕立波王丽沈兵程思
Owner JIANGSU SKYRUN PHARMA CO LTD
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