A kind of purification method of Neratinib

A technology of neratinib and purification method, which is applied in the field of neratinib purification to achieve the effect of high yield and simple operation
CN105949176BActive Publication Date: 2018-10-26ZHEJIANG HISUN PHARMA CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG HISUN PHARMA CO LTD
Publication Date
2018-10-26

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Abstract

The invention relates to a method for purifying neratinib. The method provided by the invention is capable of effectively reducing the content of impurities in neratinib and preparing high-purity neratinib, and moreover is simple in operation, high in yield and very applicable to industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry and crystallization, and in particular relates to a purification method of neratinib. Background technique

[0002] Neratinib, chemical name: (E)-N-[4-[3-chloro-4-(pyridine-2-methoxy)anilino]-3-cyano-7-ethoxy Quinolin-6-yl]-4-dimethylamino-2-butenamide, the structure of which is shown in Formula 1 below. Neratinib is a drug developed by Puma Biotechnology Company of the United States for the treatment of breast cancer. It is a highly selective human epidermal growth factor receptor (EGFR) and HER-2 inhibitor. Clinical studies have shown that neratinib is significantly more effective than Roche's Herceptin in the treatment of early HER-2 positive breast cancer.

[0003]

[0004] The impurities of neratinib are very similar to the structure and properties of neratinib, and their solubility in common organic solvents is very small, making it difficult to purify and separate. WO20061...

Claims

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