Preparation method of fosfomycin amine salt

A technology of fosfomycin and ammonia salt, applied in the field of preparation of fosfomycin ammonia salt, can solve the problems of low yield, cumbersome reaction steps and the like, and achieve the effects of convenient operation, high yield and mild reaction conditions
CN102807586AActive Publication Date: 2012-12-05NORTHEAST PHARMA GRP
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NORTHEAST PHARMA GRP
Publication Date
2012-12-05

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Abstract

The invention discloses a preparation method of fosfomycin amine salt, which comprises the following steps of: in organic solvent, enabling fosfomycin phenylethylamine salt to react with isocyanate, isothiocyanate, ketene, dipolymer of isocyanate, dipolymer of isothiocyanate or dipolymer of ketene, and tromethamine; or in the organic solvent, enabling fosfomycin bistromethamine to react with isocyanate, isothiocyanate, ketene, dipolymer of isocyanate, dipolymer of isothiocyanate or dipolymer of ketene. The preparation method provided by the invention has the advantages that the fosfomycin amine salt can be prepared in one step only, a low-temperature ion exchange column is not required, the yield is high, the cost is low, the waste gas, waste water and waste residue are less, the reaction conditions are moderate, the energy consumption is low, the operation is convenient to conduct and the method is suitable for industrial production.
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Description

technical field

[0001] The present invention specifically relates to the preparation method of fosfomycin ammonium salt. Background technique

[0002] Fosfomycin trometamol (Fosfomycin trometamol), the trade name is Monuril, the chemical name is (1R,2S)-(1,2-epoxypropylene)phosphate·2-amino-2-hydroxymethyl-1, 3 propylene glycol salt (1:1), molecular formula is C 4 h 11 NO 3 .C 3 h 7 o 4 P, the molecular weight is 259.19, and the structural formula is:

[0003]

[0004] It is a white crystalline powder. Fosfomycin trometamol is a drug that has been used for the treatment of genitourinary tract infection for a long time, and the drug was first disclosed in patent EP27957 (Zambon, 1981).

[0005] Some processes using left phosphorus and right ammonium salt (CAS No. 25383-07-7, structural formula below) as reactants are well known.

[0006]

[0007] Patent EP27597 describes the reaction of fosfomycin bis tromethamine (structural formula as follows) with p-toluenes...

Claims

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