A kind of preparation method of amorphous tofacitinib citrate

A technology of tofacitinib and citric acid, which is applied in the field of pharmacy, can solve the problems of cumbersome operation, many impurities in the product, and reduced product purity and quality, and achieve the effects of simple preparation method, good stability, and low cost
CN103073552BInactive Publication Date: 2015-08-12BEIJING PHARMA GRP CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING PHARMA GRP CO LTD
Publication Date
2015-08-12
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a preparation method for amorphous tofacitinib citrate. The preparation method is simple, can easily obtain high-purity amorphous tofacitinib citrate, and is suitable for industrial application. The preparation method includes the following steps: under the temperature range between 30 DEG C and 50 DEG C, organic solvent is used for dissolving tofacitinib citrate, so that solution is produced, water which is 15 DEG C to 25 DEG C is added into the solution, so that precipitate is produced, the precipitate is put in the environment of 15 DEG C to 25 DEG C for 4 to 24 hours, and the amorphous tofacitinib citrate is then recovered.
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Description

technical field

[0001] The invention belongs to the field of pharmacy, and relates to a preparation method of amorphous tofacitinib citrate. Background technique

[0002] The chemical formula of tofacitinib citrate is 3-{(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piper Pyridin-1-yl}-3-oxopropionitrile citrate, whose structural formula is shown in formula I, is a Janus kinase (JAKs) inhibitor developed by Pfizer. On November 6, 2012, the U.S. Food and Drug Administration (FDA) approved the listing of tofacitinib citrate (Xeljanz) for moderately to severely active rheumatoid joints that have insufficient response or intolerance to methotrexate treatment Treatment of adult patients with RA.

[0003]

[0004] Formula I

[0005] Patent WO2012135338 discloses a method for preparing amorphous tofacitinib citrate, which mainly involves first salting tofacitinib free base and acetic acid to obtain tofacitinib acetate, and then tofacitinib Dissolve acetate...

Claims

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