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Preparation method of pazopanib hydrochloride

A technology of pazopanib mono-hydrochloride, which is applied in the field of drug synthesis, can solve the problems of not being able to meet the needs of medicine, and achieve the effects of improving the sticking phenomenon, less residual solvent, and low bulk density

Inactive Publication Date: 2020-03-13
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the method of Example 1C of US2008 / 0293691A1 can prepare pazopanib monohydrochloride, the product contains a lot of residual solvent acetonitrile, which cannot meet the needs of medicine

Method used

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  • Preparation method of pazopanib hydrochloride
  • Preparation method of pazopanib hydrochloride
  • Preparation method of pazopanib hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Put 100g of pazopanib monohydrochloride hydrate in 700ml of acetonitrile-water mixed solution (volume ratio 30:1), stir at 60-70°C for 8-10 hours, cool to room temperature and stir for 1-1.5 hours and filter, 70- After vacuum drying at 80°C for 17-18 hours, 95.2 g of pazopanib monohydrochloride was obtained, yield: 95.2%. GC detection showed that the residue of acetonitrile was 76 ppm, and its XRD was as follows: figure 1 , the microscope photo as figure 2 , The bulk density is 0.22g / ml.

Embodiment 2

[0018] Fully according to the operation method of implementation one, adjust the volume ratio of the acetonitrile-water mixed solution and repeat the experiment. The specific parameter adjustment and results are as follows:

[0019]

Embodiment 3

[0021] Put 100g of pazopanib monohydrochloride hydrate in 2000ml of acetonitrile-water mixed solution (volume ratio 30:1), stir at 50-60°C for 6 hours, cool to room temperature and stir for 1-1.5 hours, filter, 70-80°C After vacuum drying for 17 to 18 hours, 93.5 g of pazopanib monohydrochloride was obtained, yield: 93.5%, and GC detection showed that the residue of acetonitrile was 82 ppm, and its XRD was as follows: figure 1 .

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Abstract

The invention relates to a preparation method of pazopanib hydrochloride, and provides a preparation method of pazopanib monohydrochloride, wherein a pazopanib monohydrochloride hydrate is subjected to stirring and crystal transformation in an acetonitrile-water mixed solution, and then filtering and drying are performed to obtain pazopanib monohydrochloride. According to the invention, the preparation method has the advantages of simple process operation and high product yield, and the residual solvent of the obtained product meets the medicinal requirements.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a preparation method of pazopanib hydrochloride monohydrochloride. Background technique [0002] Renal cell carcinoma (RCC) is a common malignant tumor worldwide, and its morbidity and mortality account for about 2%-3% of systemic tumors. Among urinary system malignant tumors, its incidence rate is second only to bladder cancer, and its incidence is rising trend year by year. In recent years, targeted drugs have made great progress in the treatment of advanced RCC. Since 2005, several drugs have been approved for marketing around the world and have become the standard treatment for advanced RCC. [0003] In my country, the current incidence of RCC in males is 4.7 / 100,000, and that in females is about 3 / 100,000. The annual incidence of kidney cancer increases by about 2.5%. Drugs that have been approved by the CFDA for the treatment of RCC include sunitinib (Pfizer) and sorafil Axit...

Claims

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Application Information

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IPC IPC(8): C07D403/12
CPCC07B2200/13C07D403/12
Inventor 张金龙付振雷刘振扬张丰盈
Owner JIANGSU HANSOH PHARMA CO LTD
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