Novel sorafenib tosylate polycrystalline form and preparation method thereof

A technology of p-toluenesulfonate and p-toluenesulfonic acid, which is applied in the field of sorafenib p-toluenesulfonate polymorph A and its preparation, can solve unfavorable industrial scale-up production, cumbersome operation of polymorph I, low Temperature and other issues, to achieve the effect of simple operation, high product yield and good repeatability

Inactive Publication Date: 2013-01-02
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD +1
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Benefits of technology

This invention relates to making certain chemicals called sulfonamides that can be used against cancer cells by blocking their growth or killing them effectively. These chemotherapy drugs are effective at treating various types of blood cell tumors such as leukemia and lymphoma patients with relapsed disease. They have been developed over time through different methods like synthesis techniques, crystallography, X ray diffraction analysis, etc., which makes it possible to produce these compounds more efficiently than previous generations of drug molecules.

Problems solved by technology

This patents describes different ways how drugs like sunitinib or selanezide are used against cancer. These methods have been shown effective at killing both normal tissue and targeted neoplasms with minimal side effect on healthy ones.

Method used

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  • Novel sorafenib tosylate polycrystalline form and preparation method thereof
  • Novel sorafenib tosylate polycrystalline form and preparation method thereof
  • Novel sorafenib tosylate polycrystalline form and preparation method thereof

Examples

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Embodiment 1

[0037] Embodiment 1 Preparation of Sorafenib tosylate (I) polymorphic form A

[0038] Add 300 g of sorafenib free base, 130 g of p-toluenesulfonic acid, 2.5 L of n-propanol, and 500 mL of water into the reaction flask. Heat the system to 80 degrees within 5 hours until the system is clear. Cool to 0° C., filter the precipitated crystals, and dry thoroughly to obtain 355 g of polymorphic form A of sorafenib p-toluenesulfonate (I), with a yield of 86% and a purity of 99.9%.

Embodiment 2

[0039] The preparation of embodiment two Sorafenib tosylate (I) polymorph A

[0040] Add 300 g of sorafenib free base, 130 g of p-toluenesulfonic acid, 2.5 L of isopropanol, and 500 mL of water into the reaction flask. Heat the system to 75 degrees within 4 hours until the system is clear. Cool to 10° C., filter the precipitated crystals, and fully dry to obtain 384 g of polymorphic form A of sorafenib p-toluenesulfonate (I), with a yield of 93% and a purity of 99.9%.

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Abstract

The invention discloses a novel sorafenib tosylate polycrystalline form A and a preparation method thereof. A DSC spectrum of the crystal form comprises a transition peak at 198.0-207.5 DEG C and a melting decomposition peak at 238.5-247.5 DEG C. The invention also discloses a method for preparing the sorafenib tosylate (I) polycrystalline form A from sorafenib free base and p-toluenesulfonic acid in a mixed solvent of alcohol and water. The method has the advantages of good repeatability, simple operation, high product yield, high purity, and suitability for industrialized productions.

Description

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Claims

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Application Information

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Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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