Preparation method of tofacitinib citrate

A technology of tofacitinib and citric acid, applied in the field of preparation of tofacitinib citrate, can solve the problems of unsuitability for industrialized production, complicated post-processing, harsh synthesis conditions and the like
CN104292231AActive Publication Date: 2015-01-21SUNSHINE LAKE PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SUNSHINE LAKE PHARM CO LTD
Publication Date
2015-01-21

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Abstract

The invention relates to a method for preparing tofacitinib citrate. The method comprises the following steps: by taking N-methyl-N-((3R, 4R)-1-benzyl-4-methylpiperidine-3-yl)-7H-pyrrolo (2, 3-d) pyrimidin-4-amine as a raw material, performing hydrogenation to remove an amino protecting group, performing amidation reaction and salt-forming reaction and finally drying to obtain tofacitinib citrate. In the preparation process, after-treatment is not required, the separation of a target intermediate is not required, and only reactants need to be added sequentially. The preparation method of tofacitinib citrate provided by the invention has the advantages of simplicity in operation, high yield, mild conditions and the like, and is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of organic and pharmaceutical synthesis, and in particular relates to a preparation method of tofacitinib citrate. Background technique

[0002] PCT applications WO 2001042246 and WO 2002096909 reported a series of pyrrolo[2,3-d]pyrimidine compounds, among them, tofacitinib citrate, chemical name: 3-[(3R,4R)-4-methyl- 3-[methyl(7H-pyrrole[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropionitrile citrate, its chemical structure is as formula (I ) as shown:

[0003]

[0004] Tofacitinib citrate is an oral Janus kinase JAK-3 and JAK-1 inhibitor developed by Pfizer. Treatment of adult patients with severely active rheumatoid arthritis (RA). Clinically, tofacitinib can be used alone or in combination with methamphetamine or other slow-acting rheumatic drugs to treat rheumatoid arthritis.

[0005] Ruggeri et al. reported for the first time in their PCT application WO 2007012953 that debenzylation was pe...

Claims

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