Refining method of tofacitinib citrate

A technology of tofacitinib and purification method, applied in the field of medicine, can solve the problem of high content of maximum single impurity and total impurity, and achieve the effects of easy operation, few by-products and simple synthesis route
CN108794491AActive Publication Date: 2018-11-13SHANDONG LUOXIN PHARMA GRP HENGXIN PHARMA CO LTD +2
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG LUOXIN PHARMA GRP HENGXIN PHARMA CO LTD
Publication Date
2018-11-13

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Abstract

The invention discloses a refining method of tofacitinib citrate. The refining method comprises the following steps: (1) dissolving a tofacitinib citrate coarse product into a mixed solvent composed of methanol and butanone, and controlling the temperature at 45 to 50 DEG C till the tofacitinib citrate is completely dissolved; (2) adding active carbon for decoloration, filtering the solution, cooling filtrate at a certain cooling rate till the temperature is -10 to 0 DEG C, separating out crystals, and growing the crystals; (3) filtering the solution, washing filtered solids with methanol, anddrying the solids in vacuum to obtain the refined tofacitinib citrate. According to the refining method disclosed by the invention, the purity of the obtained tofacitinib citrate can be up to 99.9 percent or above, and the content of total impurities and the content of a single impurity are respectively controlled within 0.1 percent and 0.05 percent; the quality of a product is obviously improved; furthermore, the refining process is easy to operate and suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, in particular to a method for refining tofacitinib citrate. Background technique

[0002] Tofacitinib citrate is a new type of Janus kinase inhibitor developed by Pfizer, the trade name is Xeljanz. This product can effectively inhibit the activity of JAK1 and JAK3, and block the signal transduction of various inflammatory cytokines. Existing studies have shown that tofacitinib citrate has a good therapeutic effect on rheumatoid arthritis, ulcerative colitis, psoriasis and other inflammation-related diseases.

[0003] The chemical name of tofacitinib citrate is 3-[(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino ]piperidin-1-yl]-3-oxopropionitrile citrate has a chemical structure shown in formula I:

[0004]

[0005] There are many types of impurities contained in the prior art preparation method and the method for refining tofacitinib citrate, and the maximum single impuri...

Claims

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