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Crystal form of sorafenib tosylate, and preparation method thereof

A technology based on p-toluenesulfonic acid and fennel, which is applied in the field of medicine, can solve the problems of low crystallinity and difficulty in meeting the production requirements of industrialized large-scale industries, and achieve good fluidity, cheap solvents, and good stability Effect

Inactive Publication Date: 2015-07-08
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

CN101065360 discloses three kinds of crystals I, II, and III of sorafenib p-toluenesulfonate and corresponding preparation methods. In order to obtain stable crystals, high temperature or long-time stirring and crystal transformation are required, and the crystallinity of the obtained crystal form is not high , it is difficult to meet the production requirements of large industrialized industries

Method used

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  • Crystal form of sorafenib tosylate, and preparation method thereof
  • Crystal form of sorafenib tosylate, and preparation method thereof
  • Crystal form of sorafenib tosylate, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of Sorafenib p-Toluenesulfonate Type B Crystal

[0037] Take 10.0g of sorafenib, add 200mL of tetrahydrofuran, stir to dissolve, add 2g of activated carbon, stir for 30min, filter, cool the filtrate to -15°C, add dropwise a solution of 4.3g of p-toluenesulfonic acid monohydrate dissolved in 13mL of tetrahydrofuran, After the addition, stir and crystallize for 1 hour, filter, and rinse the filter cake with 100ml isopropyl ether to obtain crystals, which have figure 1 X-ray powder diffraction pattern shown.

Embodiment 2

[0038] Example 2 Preparation of Sorafenib p-Toluenesulfonate Type C Crystal

[0039] The crystals prepared in Example 1 were dried under reduced pressure at 60° C. for 5 hours to obtain 12.9 g of type C crystals of sorafenib p-toluenesulfonate with a purity of 99.9%. it has figure 2 X-ray powder diffraction pattern shown.

Embodiment 3

[0040] Example 3 Preparation of Amorphous Sorafenib p-toluenesulfonate

[0041] The product of Example 1 or Example 2 was dried under reduced pressure at 80° C. for 20 hours to obtain amorphous sorafenib p-toluenesulfonate with a purity of 99.87%. it has image 3 X-ray powder diffraction pattern shown.

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Abstract

The invention provides a crystal form of sorafenib tosylate, and a preparation method thereof. The X-ray powder diffraction pattern of sorafenib tosylate of crystal form B has diffraction peaks when the values of 2theta are about 7.34DEG, 18.03DEG, 20.15DEG, 20.77DEG, 22.04DEG, 22.43DEG and 23.21DEG; and the X-ray powder diffraction pattern of sorafenib tosylate of crystal form C has diffraction peaks when the values of 2theta are about 7.61DEG and 13-33DEG. The sorafenib tosylate of crystal form C is prepared through reduced pressure heating of the sorafenib tosylate of crystal form B. The invention also provides a preparation method of amorphous crystals of sorafenib tosylate through reduced pressure heating of the sorafenib tosylate of crystal form B or C. The sorafenib tosylate crystals prepared in the invention have the advantages of good stability, high crystallization purity, simple preparation process, and suitableness for industrial production.

Description

technical field [0001] The invention relates to a crystal form of sorafenib p-toluenesulfonate and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Sorafenib p-toluenesulfonate has the structure shown in formula (I), and its chemical name is 4-{4-[3-(4-chloro-3-trifluoromethyl [0003] [0004] -Phenyl)-ureide]-phenoxy}-N-methylpyridine-2-carboxylic acid methylamine p-toluenesulfonate, sorafenib was developed and marketed by Bayer and Onyx, and is an oral small molecule inhibitory cell A growth kinase inhibitor, the drug is used to treat renal cell carcinoma (RCC) and unresectable hepatocellular carcinoma (HCC). [0005] CN101052619, WO2009034308, US20130005980 disclose the preparation method of sorafenib p-toluenesulfonate. CN101065360 discloses three kinds of crystals I, II, and III of sorafenib p-toluenesulfonate and corresponding preparation methods. In order to obtain stable crystals, high temperature or long...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81C07C309/30C07C303/32A61K31/44
CPCC07D213/81C07B2200/13
Inventor 张爱明吴叔峰张喜全朱雪焱王胡博袁哲东
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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