Synthesis method of hydroxymethylenediphosphonic acid disodium salt

By employing steps of sodium hypochlorite substitution, sodium sulfite dehalogenation, acidic hydrolysis, and pyridine salt formation, combined with recrystallization, the safety and yield issues in the synthesis of disodium hydroxymethylene diphosphonate salt were resolved, achieving feasibility for industrial production and improving product purity.

CN121554504APending Publication Date: 2026-02-24JIANGSU HUAYI TECH
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Patent Information

Application Number
CN202511632232.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-11-10
Publication Date
2026-02-24

AI Technical Summary

Technical Problem

In the existing technology, the synthesis method of disodium hydroxymethylene diphosphonate has problems such as high reaction risk, low yield and difficulty in product separation, making it difficult to be applied to industrial production.

Method used

Disodium hydroxymethylene diphosphonate was prepared by a chemical reaction under mild conditions, using steps of sodium hypochlorite substitution, sodium sulfite dehalogenation, acid hydrolysis, and pyridine salt formation, combined with a recrystallization process.

Benefits of technology

This invention provides a synthesis method that is safe, has high yield, and is environmentally friendly, suitable for industrial production, improves product purity and stability, and reduces safety risks and energy consumption.

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Abstract

The invention discloses a synthesis method of hydroxymethylenediphosphonic acid disodium salt, and relates to the field of radiopharmaceuticals, the synthesis method comprises the following steps: S1, tetraisopropyl methylenediphosphonate is subjected to a substitution reaction in a sodium hypochlorite solution to obtain tetraisopropyl dichloromethylenediphosphonate; s2, carrying out a dehalogenation reaction on the tetraisopropyl dichloromethylene diphosphate in a sodium sulfite solution to obtain tetraisopropyl monochloromethylene diphosphate; s3, carrying out a hydrolysis reaction on the tetraisopropyl monochloromethylenediphosphonate, so as to obtain pyridinium monochloromethylenediphosphonate; and S4, carrying out substitution reaction on the monochloromethylenediphosphonic acid pyridinium salt to obtain the hydroxymethylenediphosphonic acid disodium salt. The adopted raw materials and reagents are wide in source, low in price and easy to obtain, high-risk or highly-toxic chemicals are not contained, the technological process is environmentally friendly, the development direction of green chemistry is met, and good industrial application prospects are achieved.
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