A preparation method of high-purity tegretol crystal form ii
By using acetone and toluene as solvents and combining primary and secondary purification methods, the problems of low purity and high cost of industrial production of ticagrelor have been solved, and high-purity ticagrelor has been prepared, which is suitable for industrial production of various dosage forms.
CN117510508BActive Publication Date: 2026-07-24JIANGSU PURUN BIO-MEDICAL CO LTD
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- JIANGSU PURUN BIO-MEDICAL CO LTD
- Filing Date
- 2023-11-14
- Publication Date
- 2026-07-24
AI Technical Summary
Technical Problem
In the existing technology, ticagrelor has low purity, high solvent toxicity, uneven crystal particles, high industrial production cost, and poor crystal stability, making it difficult to meet the needs of various dosage forms.
Method used
Using acetone and toluene as solvents, solvent residue and purity were controlled through primary and secondary purification methods. The ratio of acetone to toluene was 1:9.0–11.0 and 1:0.5–1.5:9–11, and the temperature and time were controlled to achieve the preparation of high-purity ticagrelor.
Benefits of technology
It increases the purity of ticagrelor to 99.90%, reduces production costs, has high solvent safety, is easy to recycle and reuse, has stable crystal form, and is suitable for industrial production.
✦ Generated by Eureka AI based on patent content.
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Abstract
The application discloses a preparation method of high-purity type II ticagrelor, which comprises the following two refining steps: stirring, beating and crystallization of organic solvent A and crude ticagrelor to obtain crude wet ticagrelor, wherein the organic solvent A is one or more of acetone, ethyl acetate, toluene, N,N-dimethylformamide, methanol and isooctane; the crude wet ticagrelor is dissolved in organic solvent B, and after the solution is clarified, the solution is kept at 48-52 DEG C, organic solvent C is added, and the solution is kept at 50-55 DEG C for 3 hours, and then the solution is cooled and stirred to obtain refined ticagrelor; the organic solvents B and C are one or a mixture of both of acetone and toluene. The method is simple and easy to control, the solvent has low toxicity and easy-to-control residue, the solvent is easy to recycle and reuse, and the production cost is reduced. The purity of the product refined by the method is as high as 99.9%, and the method has wide industrial application prospect.
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