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Process for preparing strontium ranelate tetrahydrate

A technology of strontium ranelate and tetrahydrate, which is applied in the field of preparation of strontium ranelate tetrahydrate, can solve problems such as difficulty in dissolution, unexplained chemical purity, easy moisture absorption and weathering of strontium ranelate, etc. Achieve high stability, high chemical purity and simple operation

Inactive Publication Date: 2007-07-11
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The synthesis and use of strontium ranelate are described in the patent document EP0415850, but the chemical purity is not specified. In fact, according to the result of the synthesis method described in the document, the purity of the obtained product generally cannot exceed 95%.
And in concrete application, it is unsuitable as the purposes of the compound that purity is less than 99% and content is less than 98% as pharmaceutical active ingredient, in view of strontium ranelate is all difficult to dissolve in various types of solvents (it is in water, alcohol, Esters, ketones, nitriles, aromatic hydrocarbons, alkyl halides, DMF, DMSO, etc. are all insoluble) and strontium ranelate crude product is easy to absorb moisture and weathering, relatively unstable fact, it is necessary to further improve its purity when synthesizing strontium ranelate content, and to improve its stability

Method used

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  • Process for preparing strontium ranelate tetrahydrate
  • Process for preparing strontium ranelate tetrahydrate

Examples

Experimental program
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Effect test

Embodiment 1

[0015] Pour strontium ranelate tetrahydrate (30.0g, 43.6mmol, content 85%) and 100ml deionized water into the reaction flask, stir and suspend at 25°C, add dropwise 6N sulfuric acid solution to adjust the pH=1.0, the solid is completely dissolved, and the obtained The clear liquid was washed with ethyl acetate (30ml×3) times, the layers were separated, the water layer was filtered, 6N sodium hydroxide solution was added dropwise to the filtrate to adjust the pH=9.0, stirred at room temperature for 3h, filtered, the solid was washed with acetone (30ml×2) Wash and dry under reduced pressure to obtain 19.1 g of strontium ranelate tetrahydrate (yield: 75%, purity: 99.2%, content: 98.9%).

Embodiment 2

[0017] Pour strontium ranelate tetrahydrate (30.0 g, 42.1 mmol, content 82%) and 100 ml of deionized water into a reaction flask, heat to 40-50 ° C and add 6N hydrochloric acid solution dropwise to adjust pH=2.0, and the solid is completely dissolved. The obtained clear solution was washed with ethyl acetate (30ml×3) times, the layers were separated, the water layer was filtered, 10% ammonia solution was added dropwise to the filtrate to adjust the pH=10.0, stirred at room temperature for 5h, filtered, and the solid was washed with acetone (30ml×2 ), and dried under reduced pressure to obtain 19.7 g of strontium ranelate tetrahydrate (yield: 80%, purity: 99.4%, content: 99.2%).

Embodiment 3

[0019] Pour strontium ranelate tetrahydrate (30.0g, 44.6mmol, content 87%) and 100ml of deionized water into the reaction flask, heat to 40-50°C, add 6N hydrochloric acid solution dropwise to adjust the pH=3.0, and the solid is completely dissolved to obtain The supernatant liquid was washed with ethyl acetate (30ml×3) times, the layers were separated, the water layer was filtered, and saturated sodium carbonate solution was added dropwise to the filtrate to adjust the pH=8.0, stirred at room temperature for 4h, filtered, and the solid was washed with acetone (30ml×2) Wash and dry under reduced pressure to obtain 20.1 g of strontium ranelate tetrahydrate (yield: 77%, purity: 99.4%, content: 99.1%).

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Abstract

The invention discloses a making method of ranimycin strontium tetrahydrate, which comprises the following steps: adopting rough product of ranimycin strontium tetrahydrate with content over 80% as formula (I) as raw material; suspending in the water; adjusting pH value under indoor temperature or heating condition through acid until dissolving completely; obtaining the supernatant; washing through organic solvent; filtering; adjusting pH value through alkaline to neutral alkali-bias; stirring; filtering; drying to obtain the product with stable property.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of strontium ranelate tetrahydrate. Background technique [0002] Strontium ranelate is indicated to reduce the risk of new vertebral fractures (with or without fragility fractures at baseline) and hip fractures in postmenopausal women with osteoporosis. The drug can both inhibit bone resorption and promote bone formation (promoting bone formation is the most valuable way to treat osteoporosis), and has a positive effect on reducing the risk of fractures and enhancing bone strength and bone density (compared with placebo It can reduce the risk of vertebral fracture by 41% to 49%, and increase the bone mineral density of the spine by 6.8%). The drug is well tolerated. [0003] The synthesis and use of strontium ranelate are described in the patent document EP0415850, but the chemical purity is not specified. Actually, according to the synthesis method descr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D333/38
Inventor 袁哲东王强潘红娟朱雪焱
Owner SHANGHAI INST OF PHARMA IND CO LTD
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