Synthesis method of fosfomycin intermediate levo-phosphorus dextro-amine salt

Abstract

The invention relates to the technical field of compound preparation, and discloses a synthesis method of fosfomycin intermediate levo-phosphorus dextro-amine salt, which comprises the following steps: carrying out esterification reaction by using propargyl alcohol as a raw material, carrying out hydrogenation on the obtained reaction solution, Pt / C and Cu (II) EDTA to prepare cis-propenyl phosphorus oxychloride solution, hydrolyzing, regulating the pH value of the reaction solution by using ammonia gas, reacting with R-(+)-alpha-phenylethylamine to form salt, and epoxidizing to obtain the fosfomycin intermediate levo-phosphorus dextro-amine salt. And performing post-treatment to obtain the product. The propargyl alcohol is not hydrolyzed after esterification, so that generation of impurity propadiene phosphate is reduced, and cis-propenyl phosphoric acid with higher purity can be obtained through later hydrogenation; the hydrolysis step after esterification is omitted, a large amount of water does not need to be distilled and concentrated, and energy consumption is reduced; the reaction temperature and the hydrogen pressure in the hydrogenation step are relatively low, and the reaction safety is relatively high; r-(+)-alpha-phenylethylamine is used in the epoxidation stage, and splitting operation is not needed, so that the process is simplified; all the used solvents can be recycled and reused, so that the method is environment-friendly.

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