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High-yield piperaquine preparation method

A high-yield, piperaquine technology, applied in the field of preparation of anti-malarial drugs, can solve the problems of low purity of piperaquine, low total yield, high cost, etc., achieve the elimination of nausea and vomiting side effects, reduce the total amount of medication, and reduce production costs low effect

Inactive Publication Date: 2019-03-08
ARTEPHARM CO LTD CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method has complex process, high energy consumption, high cost, and the generated piperaquine has low purity and low total yield
Among them, anhydrous piperazine is decomposed by heat to release toxic gas, which is corrosive, harmful to human health, and flammable and explosive.
In addition, 1,3-bromochloropropane is a flammable and highly irritating substance. Mistake, contact with skin or inhalation of vapor is harmful to the body, pollutes the atmosphere and water, and has strong destructive power to the ozone layer.
Therefore, the risk coefficient of the whole reaction process of the preparation method is high, and it is easy to cause environmental pollution

Method used

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  • High-yield piperaquine preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] First, calculate the amount of raw materials according to the obtained amount of piperaquine theory of 535.56g (i.e. the amount of 1mol); specifically, add 15071g of purified water in a 40L dissolution tank, heat to 70°C, and then weigh 753.56g of piperaquine hydrochloride (i.e. 1mol) into hot water, stirred, then heated to 85 ° C to completely dissolve piperaquine hydrochloride, and filtered to obtain piperaquine hydrochloride solution.

[0025] Next, take by weighing the ammoniacal liquor 420g (being the amount of 3mol) that concentration is 25%, slowly join in the above-mentioned obtained piperaquine hydrochloride solution, stir while adding, and reaction temperature is controlled at 70~80 ℃, after adding Continue to stir for 4 minutes, after the reaction, the piperaquine precipitate can be obtained by centrifugal filtration.

[0026] Finally, the obtained piperaquine precipitate was washed repeatedly with purified water twice until the residual hydrochloride in the ...

Embodiment 2

[0028] First, calculate the amount of raw materials according to the obtained amount of piperaquine theory of 535.56g (that is, the amount of 1mol); specifically, add 22607g of purified water to a 40L dissolution tank, heat to 70°C, and then weigh 753.56g of piperaquine hydrochloride (that is, 1mol amount) into hot water, stirred, then heated to 90 ° C to completely dissolve piperaquine hydrochloride, and filtered to obtain piperaquine hydrochloride solution.

[0029] Next, take by weighing the ammoniacal liquor 560g (being the amount of 4mol) that concentration is 25%, slowly join in the above-mentioned obtained piperaquine hydrochloride solution, stir while adding, and reaction temperature is controlled at 70~80 ℃, after adding Continue to stir for 4 minutes, after the reaction, the piperaquine precipitate can be obtained by centrifugal filtration.

[0030] Finally, the obtained piperaquine precipitate was repeatedly washed with purified water for 3 times until the residual ...

Embodiment 3

[0032] First, calculate the amount of raw materials according to the obtained amount of piperaquine theory of 535.56g (that is, the amount of 1mol); specifically, add 30142g of purified water to a 40L dissolution tank, heat to 70°C, and then weigh 753.56g of piperaquine hydrochloride (that is, 1mol amount) into hot water, stirred, then heated to 95 ° C to completely dissolve piperaquine hydrochloride, and filtered to obtain piperaquine hydrochloride solution.

[0033] Next, take by weighing the ammoniacal liquor 700g (being the amount of 5mol) that concentration is 25%, slowly join in the above-mentioned obtained piperaquine hydrochloride solution, stir while adding, and reaction temperature is controlled at 70~80 ℃, after adding Continue to stir for 4 minutes, after the reaction, the piperaquine precipitate can be obtained by centrifugal filtration.

[0034] Finally, the obtained piperaquine precipitate was repeatedly washed with purified water for 4 times until the residual ...

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Abstract

The invention discloses a high-yield piperaquine preparation method and belongs to the technical field of anti-malarial medicine preparation. The preparation method comprises the following steps: firstly, utilizing piperaquine hydrochloride as a starting material, adding hot water, stirring to completely dissolve the starting material while heating the starting material and filtering to obtain a piperaquine hydrochloride solution; then, adding ammonium hydroxide into the obtained piperaquine hydrochloride solution to perform neutral reaction and filtering to obtain piperaquine precipitate; finally, adding purified water into the obtained piperaquine precipitate and repeatedly washing, dewatering and drying to obtain piperaquine. According to the preparation method disclosed by the invention, the piperaquine hydrochloride is utilized as the starting material to directly perform neutral reaction with ammonium hydroxide to obtain piperaquine through one-step transformation. As the piperaquine is insoluble in water, the piperaquine is easy to separate and purify and has the advantages of small impurities, high purity and high product yield. In addition, the technical scheme of the preparation method disclosed by the invention further avoids use of toxic reagents and has the advantages of small work procedures, low production cost and suitability for industrial production.

Description

technical field [0001] The invention relates to the technical field of preparation of antimalarial drugs, in particular to a method for preparing piperaquine with high yield. Background technique [0002] Malaria is a major infectious disease in the tropics and subtropics. According to the World Malaria Report 2017 released by the World Health Organization, in 2016, there were 216 million malaria cases in 91 countries, and the total number of global malaria deaths reached 445,000. The African Region still accounts for about 90% of all malaria cases and deaths worldwide. Malaria is not only a serious health problem in developing countries, but also a social problem that hinders economic development and social progress. The emergence of drug-resistant Plasmodium falciparum strains and its global spread have increased the difficulty of malaria control and made the situation of global malaria control increasingly severe. Plasmodium falciparum develops resistance to drugs, whi...

Claims

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Application Information

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IPC IPC(8): C07D215/46
CPCC07D215/46
Inventor 杨兆丽张志坚张加颂罗楚彪
Owner ARTEPHARM CO LTD CHINA
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