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1-Acetamidoethylidene-1,1-diphosphonate and its preparation method and application

A technology of acetamide group and bisphosphonic acid trisodium salt, which is applied in the field of medicine, can solve the problems of unsatisfactory excretion effect, high toxicity, and poor pertinence, etc., achieve excellent excretion effect, stable properties, and ensure product purity Effect

Active Publication Date: 2019-08-23
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, for radioactive strontium, there are 1-acetamidopropylidene-1,1-diphosphonic acid (S-186) and 1-propionamidoethylidene-1,1-diphosphonic acid (S-186). -106), etc., but these drugs alone have unsatisfactory effects on promoting excretion, and are more toxic (Luo Meichu, S106, S86 on the effect of radioactive strontium on promoting excretion, Radiation Protection, 1984 (3): 63-67)
Although the nano-drug expulsion-promoting agents studied in recent years have certain effects, there are still problems such as lack of pertinence (Shu Hongzao, Preparation of chitosan-ethylenediaminetetraacetic acid nanoparticles and mice ~(89)Sr~(2 +) Research on the effect of excretion, Suzhou University Journal (Medical Science), 2010,30(5):982-986)

Method used

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  • 1-Acetamidoethylidene-1,1-diphosphonate and its preparation method and application
  • 1-Acetamidoethylidene-1,1-diphosphonate and its preparation method and application
  • 1-Acetamidoethylidene-1,1-diphosphonate and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of 1-acetamidoethylidene-1,1-diphosphonic acid calcium sodium salt

[0036] The synthetic route is as follows:

[0037]

[0038] The preparation process is as follows:

[0039] 1.1 Synthesis of ethylamine-1,1-diphosphonic acid

[0040]

[0041] Phosphorous acid (1100 g, 13.4 mol) was heated to 150° C., and acetonitrile (18 mL, 3.4 mol) was added dropwise within 0.5 h with stirring. After reacting overnight, the reaction mixture turned into a white cake. Cool, add methanol, stir, and turn into a paste. Filtration and drying gave a white powder, namely ethylamine-1,1-diphosphonic acid (482 g, yield 69%), melting point>200°C.

[0042] 1.2 Synthesis of ethylamine-1,1-diphosphonic acid trisodium salt

[0043]

[0044] Ethylamine-1,1-diphosphonic acid (600.00 g, 2.9 mol) was weighed and dissolved in 10 L of water, and magnetically stirred to form a suspension. NaOH (351 g, 8.7 mol) was dissolved in 1 L of water, and slowly added dropwise ...

Embodiment 2

[0052] Example 2: Study on the physicochemical properties of calcium sodium salt of 1-acetamidoethylidene-1,1-diphosphonate

[0053] 2.1 Physicochemical properties of calcium sodium salt of 1-acetamidoethylidene-1,1-diphosphonate

[0054] Properties: White or off-white loose lump or powder.

[0055] Identification of phosphorus, calcium and sodium:

[0056] ①Take 10 mg of sample (calcium sodium salt of 1-acetamidoethylidene-1,1-diphosphonate, the same below) and dissolve it in 2 mL of water, add SnCl 2 2 drops of aqueous solution, showing blue. The principle is that the sample is subjected to SnCl 2 Phosphorus is released after reduction, and ammonium molybdate test solution is added to form "molybdenum blue".

[0057] ②Take 10 mg of the sample and add 2 mL of water to dissolve it, check the calcium salt according to the appendix of the Pharmacopoeia 2005 edition, and add ammonium oxalate test solution to form a white precipitate. The principle is that the calcium salt in...

Embodiment 3

[0083] Example 3: The effect of 1-acetamidoethylidene-1,1-diphosphonic acid calcium sodium salt on the excretion of radioactive strontium

[0084] 3.1 Experimental materials and methods

[0085] Material:

[0086] Wistar rats, weighing 130-180 g.

[0087] Radionuclide, irradiated SrCO 3 pink( 85+89 SrCO 3 There are a lot of carriers). Irradiated SrCO 3 Specific activity 5 ~ 10mCi / g, first dissolved with dilute hydrochloric acid, and then diluted.

[0088] Evacuator, calcium sodium salt of 1-acetamidoethylidene-1,1-diphosphonate, and calcium bis(diaminoethyl)ether tetraacetate (BADE-Ca, Shanghai Institute of Materia Medica, Chinese Academy of Sciences) for comparison , Diethylaminosulfide tetraacetic acid (BADS, Shanghai Institute of Materia Medica, Chinese Academy of Sciences). Wherein BADE and BADS are considered to be two complexing agents with good strontium-expelling effect in foreign animal experiments (SlatB et al. -5), BADE-Ca (BAETA-Ca) has been used in human ...

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Abstract

The invention discloses a 1-acetamido-ethylidene-1,1-bisphosphonate, and particularly discloses a 1-acetamido-ethylidene-1,1-calcium diphosphate. A structural formula of the 1-acetamido-ethylidene-1,1-bisphosphonate is as shown in a formula (I). The invention further discloses a preparation method of the compound in the formula (I). The compound in the formula (I) has an anti-radiation effect, especially has an excellent discharge-facilitating effect on strontium, is stable in property and good in water solubility, and can be used as a high-efficiency and low-toxicity discharge-facilitating drug for pollution in radioactive strontium.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to 1-acetamidoethylidene-1,1-diphosphonate and its preparation method and application. Background technique [0002] Radioactive strontium is one of the main products of nuclear fission, and is the most harmful nuclide in late-stage radioactive fallout. During nuclear attacks, nuclear terrorism, and nuclear accidents, radioactive strontium mainly causes bone internal irradiation damage, resulting in abnormal hematopoietic function and regeneration disorders. Sexual anemia, diffuse osteoporosis or fractures, etc. If it is not excreted for a long time, it can also induce malignant tumors such as osteosarcoma and leukemia. [0003] At present, the excretion-promoting drugs available at home and abroad (such as "cuipailing injection") only have excretion-promoting effects on radioactive nuclides such as lanthanum, praseodymium, neodymium, zirconium, niobium, etc., and have almost no ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/38A61P39/02A61P39/00
Inventor 高福杨彦勇蔡建明李百龙赵海男程赢刘聪崔建国陈媛媛
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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