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Crystal form of Brelocitinib tosilate as well as preparation method and application of crystal form of Brelocitinib tosilate

A technology of toluene sulfonate and toluene sulfonic acid, which is applied in the preparation of sulfonate, preparation of organic compounds, chemical instruments and methods, etc. It can solve problems such as poor tablet compression, extremely high preparation process requirements, and difficult processes

Pending Publication Date: 2022-08-02
SOLIPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Furthermore, the use of a solid form with high hygroscopicity will lead to many problems after the preparation is made, such as: unsealing, bottle opening stability; extremely high preparation process requirements; affecting dissolution, which will easily lead to increased impurities; poor tablet compression, difficult process Large; and poor liquidity, etc.

Method used

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  • Crystal form of Brelocitinib tosilate as well as preparation method and application of crystal form of Brelocitinib tosilate
  • Crystal form of Brelocitinib tosilate as well as preparation method and application of crystal form of Brelocitinib tosilate
  • Crystal form of Brelocitinib tosilate as well as preparation method and application of crystal form of Brelocitinib tosilate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Take 39 g of brepocitinib and dissolve it in 200 mL of acetonitrile by ultrasonic, and take another 17.2 g of toluenesulfonic acid and dissolve it in 25 mL of water by ultrasonic, add the aqueous solution of toluenesulfonic acid dropwise to the acetonitrile solution of brepocitinib (positive addition), stir at room temperature overnight, and precipitate a solid After centrifugation, it was vacuum-dried at room temperature for 24 hours to obtain 46 g of brepocitinib tosylate crystal form 1.

[0089] Measured by XRPD (X-ray powder diffractometer), the XRPD pattern of the brepocitinib tosylate crystal form 1 expressed at 2θ angle, as shown in figure 1 shown.

[0090] The TGA characterization data of Brepocitinib tosylate crystal form 1 are: before 100 °C, the weight loss is 0.26%, the decomposition temperature is about 281 °C, and it is anhydrous, such as figure 2 shown.

[0091] The DSC characterization data of Brepocitinib tosylate crystal form 1 are: Onset value is 2...

Embodiment 2

[0097] Take 15mg brepocitinib in 1mL of isopropanol to dissolve by ultrasonic, and take another 66.35mg of toluenesulfonic acid to dissolve in 5mL of isopropanol by ultrasonic, and add 0.7mL of toluenesulfonic acid in isopropanol solution dropwise to brepocitinib in isopropanol solution (positive addition), stirred at room temperature, and immediately after the solid was precipitated, centrifuged, and vacuum-dried at room temperature for 24 hours to obtain brepocitinib tosylate crystal form 1.

Embodiment 3

[0099] Take 60 mg of brepocitinib and dissolve it in 0.2 mL of acetone by ultrasonic, and take another 26.54 mg of toluenesulfonic acid and dissolve it in 1.29 mL of acetone by ultrasonic. Add the acetone solution of toluenesulfonic acid dropwise to the acetone solution of brepocitinib (positive addition), and stir at room temperature. Immediately after precipitation of solid, centrifugation, and vacuum drying at room temperature for 24 hours to obtain brepocitinib tosylate crystal form 1.

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Abstract

The invention provides a Brelocitinib tosilate crystal form as well as a preparation method, a pharmaceutical composition and application of the Brelocitinib tosilate crystal form. Compared with the known Brelocitinib compound, the Brelocitinib toluenesulfonate disclosed by the invention is a Brelocitinib toluenesulfonic acid crystal form 1 with good physicochemical properties, and compared with an amorphous form, the Brelocitinib toluenesulfonate is more favorable for being prepared into a preparation product and is suitable for industrial production.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry. Specifically, the present application relates to the crystalline form of brepocitinib tosylate and its preparation method and use. Background technique [0002] Brepocitinib, with the development code PF-06700841, is a selective tyrosine kinase 2 (TYK2) and Janus kinase 1 (JAK1) inhibitor developed by Pfizer for the treatment of psoriasis and atopic dermatitis (AD). Topical therapy, as well as psoriasis, psoriatic arthritis (PA), inflammatory bowel disease (IBD), Crohn's disease (CD), ulcerative colitis (UC), vitiligo (eg active non-segmental Vitiligo), systemic lupus erythematosus (SLE), aplastic anemia (AA) and hidradenitis suppurativa (HS), etc. The chemical name for Brepocitinib is: [(1S)-2,2-difluorocyclopropyl]-[(1R,5S)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3 ,8-diazabicyclo[3.2.1]octan-8-yl]methanone, its structural formula is shown in the following formula (I): ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/08C07C309/30C07C303/44C07C303/32A61K31/506A61P17/00A61P19/02A61P17/06A61P1/00A61P1/04A61P17/14A61P29/00
CPCC07D487/08C07C309/30A61P17/00A61P19/02A61P17/06A61P1/00A61P1/04A61P17/14A61P29/00C07B2200/13A61K31/506C07C303/32C07C303/44A61P37/00
Inventor 盛晓红盛晓霞彭晨玥
Owner SOLIPHARMA
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