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Aminophosphonic acid compound for nuclear medicine and its preparing process

An aminophosphonic acid and nuclear medicine technology, applied in the field of preparation of aminophosphonic acid compounds, can solve the problems of low yield, harsh reaction conditions and the like, and achieve the effects of high yield, easy reaction conditions, and simple operation of the preparation process

Inactive Publication Date: 2002-09-18
INST OF NUCLEAR PHYSICS & CHEM CHINA ACADEMY OF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aminophosphonic acid compounds used in nuclear medicine prepared by conventional methods have harsh reaction conditions and low yields

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Synthetic method of HEDTMP

[0038] Add 26 grams of hydroxyethylethylenediamine, 64 milliliters of concentrated hydrochloric acid, and 61 grams of phosphorous acid into a 300 milliliter three-necked bottle equipped with a condensing reflux tube, a stirrer and a constant pressure sampler, and stir the mixture in a water bath, then a water bath The temperature is 80±5°C, and then 61 ml of 36% formaldehyde aqueous solution is slowly added dropwise from a constant pressure injector, and the dropwise addition is completed in 15 minutes. The mixed solution was reacted in a water bath at 80±5° C. for 4 hours, and then left to cool to room temperature. The product was precipitated into a yellow jelly with absolute ethanol, and the isolated yellow jelly was dissolved in warm water at 80°C. After cooling, it was precipitated and purified with absolute ethanol; Dissolved in warm water, cooled and dried in a lyophilizer to obtain a white lyophilized product with a yield of 75% (ca...

Embodiment 2

[0040] Synthetic method of HEDTMP

[0041] Add 26 grams of hydroxyethylethylenediamine, 80 milliliters of concentrated hydrochloric acid, and 80 grams of phosphorous acid into a 500-milliliter three-necked flask equipped with a condensing reflux tube, a stirrer, and a constant pressure sampler, and stir the mixture in a water bath. The temperature is 80±5°C, and then 100 ml of 36% formaldehyde aqueous solution is slowly added dropwise from a constant pressure injector, and the dropwise addition is completed in 20 minutes. The mixed solution was reacted in a water bath at 60±5° C. for 4 hours, and then left to cool to room temperature. The product was precipitated into a yellow jelly with absolute ethanol, and the isolated yellow jelly was dissolved in warm water at 80°C. After cooling, it was precipitated and purified with absolute ethanol; Dissolved in warm water, cooled and dried in a freeze dryer to obtain a white freeze-dried product with a yield of 80% (calculated as ami...

Embodiment 3

[0043] Synthetic method of HEDTMP

[0044] Add 26 grams of hydroxyethylethylenediamine, 120 milliliters of concentrated hydrochloric acid, and 65 grams of phosphorous acid into a 500-milliliter three-necked flask equipped with a condensing reflux tube, a stirrer, and a constant pressure sampler, and stir the mixture in a water bath. The temperature is 80±5°C, and then 65 ml of 36% formaldehyde aqueous solution is slowly added dropwise from a constant pressure injector, and the dropwise addition is completed in 15 minutes. The mixed solution was reacted in a water bath at 80±5° C. for 4 hours, and then left to cool to room temperature. The product was precipitated into a yellow jelly with absolute ethanol, and the isolated yellow jelly was dissolved in warm water at 80°C. After cooling, it was precipitated and purified with absolute ethanol; Dissolved in warm water, cooled and dried in a lyophilizer to obtain a white lyophilized product with a yield of 85% (calculated as amine...

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PUM

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Abstract

An aminophosphonic acid compound used for nuclear medicine is prepared through adding amine and phosphoruc acid to reactor, dropping concentrated acid and formaldehyde, reaction, cooling, and precipitation in water or absolute alcohol. It along with Tc, Re, Or Sm can be used to prepare medicine for treating cancers.

Description

1. Technical field [0001] The invention belongs to the field of organic chemical synthesis, and in particular relates to a preparation method of an aminophosphonic acid compound used in nuclear medicine. 2. Background technology [0002] Due to the pollution and destruction of the human living environment and the aging of the population, the incidence and mortality of malignant tumors are increasing year by year, which has attracted the attention of the world. According to the report of the World Health Organization, there are 10 million new cancer cases and 6.6 million deaths in the world every year. There will be 300 million new cases of cancer in the next 25 years and there will be 100 million deaths. The incidence of bone metastases is very high, about 35-40 times that of primary bone tumors. Malignant tumors in almost any organ can metastasize to bone. Autopsy confirmed that 50% of cancer patients have bone metastasis, and the bone metastasis rate of breast cancer, l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/38
Inventor 蒋树斌罗顺忠刘国平蒲满飞何佳恒邴文增
Owner INST OF NUCLEAR PHYSICS & CHEM CHINA ACADEMY OF
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