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Purification and preparation methods of ticagrelor

A technology of ticagrelor and purification method, which is applied in the field of purification and preparation of ticagrelor, which can solve the problems of cumbersome operation steps and unrecyclable reagents, and achieve the effects of expanding the scope of use, facilitating industrial realization, and saving resources

Inactive Publication Date: 2017-06-20
SHAANXI BICON PHARMA GRP HLDG COMPANY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing purification method of ticagrelor has the disadvantages that the reagents cannot be recycled and the operation steps are very cumbersome.

Method used

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Examples

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Effect test

preparation example Construction

[0037] A method for preparing ticagrelor, including the existing method for preparing crude ticagrelor and the above-mentioned method for purifying ticagrelor. The prepared crude ticagrelor with low purity and containing a large amount of impurities is purified to obtain a high-purity refined product of ticagrelor. The purity of the prepared ticagrelor is improved.

[0038] The invention discloses a purification method of ticagrelor. The raw material source of the method is wide, the price is cheap, and the reaction conditions are easy to realize and obtain. The operation process of the method is simple and easy to control, and has great potential application value in industrial production. The method only uses one solvent—ethyl acetate to purify the crude ticagrelor product, reduces the types of solvents used, and reduces the waste of solvents by not using combined solvents. After the ethyl acetate is used, the ethyl acetate can be recycled to further save resources and red...

Embodiment 1

[0041] 20 g of crude ticagrelor (HPLC content 84.3%) was mixed with 360 ml of ethyl acetate, stirred and dissolved at 25° C. for 7 hours, and the stirring was stopped after it was completely dissolved. After cooling at 20°C for 6 hours, the mixture was cooled at -20°C for 22 hours to precipitate ticagrelor crystals. Filter, use 10ml of ethyl acetate to wash the ticagrelor crystals twice, then put the ticagrelor crystals into a vacuum drying oven to dry, the drying conditions of the first stage are set to 0.08Mpa, 37°C, and dry for 5 hours ; The drying conditions of the second stage were set at 0.095Mpa, 45°C, and dried for 7 hours, and the yield was 92.1%. The ticagrelor crystals obtained after drying were detected by HPLC, and the content was 99.76%.

Embodiment 2

[0043] Compared with Embodiment 1, the operating steps of this embodiment are basically the same, the difference is that the operating conditions of each step are changed. The amount of ethyl acetate used in this example was 7 times the amount of ticagrelor, the temperature for stirring and dissolving was 40° C., and the dissolving time was 5 hours. The temperature of the first cooling is 25°C, and the cooling time is 8 hours; the temperature of the second cooling is -15°C, and the cooling time is 20 hours. The number of times of rinsing is 3 times, and the amount of ethyl acetate used for rinsing is 20 ml. The first drying condition is 0.084Mpa, 35°C for 7 hours, and the second drying condition is 0.09Mpa, 40°C for 8 hours. The yield was 95.5%, and the result detected by HPLC was 99.65%.

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PUM

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Abstract

The invention relates to the field of pharmacy and in particular relates to purification and preparation methods of ticagrelor. The purification method of the ticagrelor comprises the following steps: mixing the ticagrelor and ethyl acetate at the ratio ranging from (1g to 3ml) to (1g to 20ml) and dissolving to obtain a mixed solution; after cooling the mixed solution, filtering to obtain a ticagrelor crystal; drying the ticagrelor crystal. The preparation method of the ticagrelor comprises the purification method of the ticagrelor. According to the purification method, only one single solvent is used for purifying and purification operation is simple; the solvent can be recycled so that resources are saved and a whole purification process is simple and practical.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a method for purifying and preparing ticagrelor. Background technique [0002] Ticagrelor, also known as ticagrelor, is a new type of selective small molecule anticoagulant drug developed by AstraZeneca. Ticagrelor reversibly acts on the purine 2 receptor (purinoceptor2, P2) subtype P2Y12 on vascular smooth muscle cells (VSMC), does not require metabolic activation, and significantly inhibits platelet aggregation induced by adenosine diphosphate (ADP) Effect, and rapid onset after oral administration, can effectively improve the symptoms of patients with acute coronary heart disease. [0003] With the continuous deepening of clinical application, the demand for its raw materials is increasing. There have been a lot of reports on its synthetic methods in China, but among the reported synthetic methods, the treatment method for crude ticagrelor hydrochloride is very complicated. The exis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04Y02P20/582
Inventor 陈雪荣
Owner SHAANXI BICON PHARMA GRP HLDG COMPANY
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