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Preparation method of sodium ibandronate monohydrate

A technology of sodium ibandronate and monohydrate, applied in the field of preparation of sodium ibandronate monohydrate, to achieve the effects of avoiding genotoxic substances, high yield, avoiding patent protection and solvation problems

Inactive Publication Date: 2015-01-14
湖北华世通生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is easy to form solvent compounds by ethanol purification, and at the same time, it is possible to obtain genotoxic impurities with limited structure in terms of the possibility of reaction

Method used

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  • Preparation method of sodium ibandronate monohydrate
  • Preparation method of sodium ibandronate monohydrate
  • Preparation method of sodium ibandronate monohydrate

Examples

Experimental program
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Embodiment 1

[0019] Add 40.0g of aminopropionate hydrochloride, 31.0±1g of phosphite, and 153.0g of toluene into the reactor, heat to T=70-75°C, keep stirring at this temperature and slowly add 26.0g of phosphorus trichloride dropwise. T=85-95°C Stir the reaction to complete, slowly lower the temperature of the reactor to T=20-40°C, separate and discard the toluene layer. Then add toluene into the reactor, stir, and discard the toluene layer. Drinking water was added to the reactor, and the reaction was stirred for an hour. The filtrate was concentrated to give an oil. Add purified water to the oil, and slowly add saturated sodium hydroxide solution to adjust the pH value of the solution to 4.0-4.6. Acetone was slowly added dropwise, a large amount of solids precipitated, the material was put into a suction filtration funnel, and suction filtered to obtain crude ibandronate sodium.

[0020] Add the crude sodium ibandronate and purified water (crude sodium ibandronate: purified water = 1...

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PUM

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Abstract

The invention discloses a preparation method of sodium ibandronate monohydrate. The method is characterized by comprising the following steps: adding 3-(N-methyl-n-pentylamine) propionic acid hydrochloride, phosphorous acid and phosphorus trichloride to solvent methylbenzene to react, so as to obtain an ibandronic acid ester; hydrolyzing to obtain ibandronic acid and salifying with sodium hydroxide; and after refining, adding water to concentrate, so as to obtain sodium ibandronate monohydrate. According to the process, genotoxic substances which can be generated can be well avoided, and the yield is high. By adoption of a water concentration method, the problems of patent protection and solvation can be well avoided, so as to obtain stable monohydrate.

Description

technical field [0001] The invention belongs to the field of pharmaceutical synthesis and production, and in particular relates to a preparation method of sodium ibandronate monohydrate. Background technique [0002] Sodium ibandronate is a bone resorption inhibitor developed by Roche, Switzerland. It was first launched in Germany and Austria in 1996 and is mainly used to treat hypercalcemia caused by malignant tumors. Its function is to inhibit bone resorption. It can not only inhibit the activity and maturation of osteoclasts, but also induce apoptosis of osteoclasts, thereby blocking the increase of bone resorption caused by various reasons, and can effectively prevent the occurrence of bone metastasis. It has the advantages of high efficiency, low toxicity and convenient use. It is currently the most widely indicated bisphosphonate drug. [0003] Sodium Ibandronate Chemical name: 1-Hydroxy-3-(N-methyl-pentylamino)-propylene diphosphonic acid monosodium salt monohydrate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/38C07F9/40
Inventor 陶令峰
Owner 湖北华世通生物医药科技有限公司
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