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Preparation method of strontium ranelate

A technology of strontium ranelate and strontium salt, which is applied in the field of preparation of strontium ranelate and its hydrate, can solve the problems of easy decarboxylation, difficult quality control, difficult to meet the purity requirements, and achieve high content and controllable product quality , the effect of simple operation

Inactive Publication Date: 2013-12-25
YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent discloses three preparation methods: the first preparation method is the direct hydrolysis of ranelate tetraester and strontium hydroxide to obtain strontium ranelate, which is difficult to purify; the second method is ranelate The acid tetraester is hydrolyzed in sodium hydroxide solution, and the obtained sodium ranelate is treated with ion exchange resin to obtain ranelic acid, which is then salted with strontium chloride in water to prepare strontium ranelate. In this method, ranelic acid does not Stable, easy to decarboxylate, quality is difficult to control; the third method is hydrolysis of ranelate tetraester in sodium hydroxide solution, the gained sodium ranelate is washed with a large amount of ethanol, and then becomes strontium ranelate with strontium chloride. Using a large amount of ethanol while sodium ranelate is only washed, the purity is difficult to meet the requirements

Method used

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  • Preparation method of strontium ranelate
  • Preparation method of strontium ranelate
  • Preparation method of strontium ranelate

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Add 0.6KG tetraethyl ranelate, 5L ethanol, and potassium hydroxide aqueous solution (0.31KG potassium hydroxide dissolved in 3L water) to a 10L reactor, heat to reflux, and react for 4 hours. The solvent was removed from the reaction solution to obtain 0.91KG of a light yellow viscous substance. Add 3.6L of water / methanol (volume ratio 1:7) mixed solution, heat to dissolve to obtain a brownish-yellow solution, cool down and wash, filter to obtain 0.44KG sodium ranelate refined product, yield 67.4%.

[0026] Dissolve potassium ranelate 0.44KG in 1.8L water, heat to reflux, add aqueous strontium chloride solution (0.37Kg dissolved in 2.5KG water) and continue to reflux for 2 hours, heat filter, dry to obtain strontium ranelate hydrate 0.51KG, and collect The rate is 87.2%. Content 98.6%, maximum impurity 0.05%.

Embodiment 2

[0028] Add 0.6KG tetraethyl ranelate, 5L ethanol, and aqueous sodium hydroxide solution (0.22KG sodium hydroxide dissolved in 3L water) to a 10L reactor, heat to reflux, and react for 4 hours. The solvent was removed from the reaction liquid to obtain 0.80KG of a light yellow viscous substance. Add 4.8 L of water / methanol (volume ratio 1:5) mixed solution, heat to dissolve to obtain a brownish-yellow solution, cool down and wash, filter to obtain 0.43KG sodium ranelate refined product, yield 75.7%.

[0029] Dissolve sodium ranelate 0.43KG in 1.8L water, heat to reflux, add strontium chloride aqueous solution (0.59Kg dissolved in 2.5KG water) and continue to reflux for 2 hours, heat filter, dry to obtain strontium ranelate hydrate 0.57KG, and collect The rate is 86.7%. Content 98.8%, maximum impurity 0.04%.

Embodiment 3

[0031] Add 0.6KG tetraethyl ranelate, 5L ethanol, and sodium hydroxide aqueous solution (0.22KG sodium hydroxide dissolved in 3L distilled water) into a 10L reactor, heat to reflux, and react for 4 hours. The solvent was removed from the reaction liquid to obtain 0.80KG of a light yellow viscous substance. Add 4.8 L of distilled water / methanol (volume ratio 1:5) mixed solution, heat to dissolve to obtain a brownish-yellow solution, cool down and wash, filter to obtain 0.44KG sodium ranelate fine product, yield 77.5%.

[0032] Dissolve sodium ranelate 0.44KG in 1.8L distilled water, heat to reflux, add strontium chloride aqueous solution (0.60Kg dissolved in 2.5KG distilled water) and continue to reflux for 2 hours, heat filter, and dry to obtain strontium ranelate hydrate 0.58KG , yield 86.2%. Content 99.7%, maximum impurity 0.03%.

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Abstract

The invention relates to a preparation method of strontium ranelate and a hydrate thereof, and the method is suitable for industrialized production. The method is as below: carrying out a hydrolysis reaction on tetra ester ranelic acid and a sodium hydroxide or potassium hydroxide solution; refining the obtained sodium ranelate or potassium ranelate with a mixed solution of water and an organic solvent to prepare high-purity sodium ranelate or potassium ranelate; and reacting the sodium ranelate or potassium ranelate with strontium salt to obtain strontium ranelate and the hydrate thereof. The strontium ranelate and the hydrate thereof prepared by the method provided by the invention has high content, maximum impurity less than 0.1% and controllable quality, and can meet the needs as a medicine active component.

Description

Technical field: [0001] The invention relates to the field of medicinal chemistry, in particular to a method for preparing strontium ranelate and a hydrate thereof suitable for industrial production. Background technique: [0002] Strontium ranelate is a new type of anti-osteoporosis drug, mainly used to treat and prevent osteoporosis in postmenopausal women, and significantly reduce the risk of vertebral fractures and hip fractures. Strontium ranelate can significantly increase bone mineral density and reduce fracture incidence in patients with osteoporosis without serious adverse reactions. It is currently the only drug that can both inhibit bone resorption and promote bone formation. It is a new anti-osteoporosis drug and has broad clinical application prospects. The dose of strontium ranelate is relatively large, 2g / day, and it needs to be taken for a long time. Therefore, it is of great practical significance to reduce impurities and production costs through process o...

Claims

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Application Information

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IPC IPC(8): C07D333/38
Inventor 张培龙石和鹏侯鹏乔野于芳吕长江薛为哲杜继航贾燕花
Owner YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA
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