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

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

CN103113408AActive Publication Date: 2013-05-22JIANGSU SKYRUN PHARMA CO LTD
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  • Novel method for preparing fosfomycin phenylethylamine
  • Novel method for preparing fosfomycin phenylethylamine

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Experimental program
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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

Patent Timeline
22 May 2013
Publication
CN103113408A
IPC
C07F9/655; C07C211/27; C07C209/68
Inventors
燕立泒; ηŽ‹δΈ½