A kind of preparation method of the intermediate of tyrosine kinase inhibitor

A tyrosine kinase and inhibitor technology, which is applied in the field of intermediate preparation, can solve the problems of many impurities, low purity, and difficulty in purification, and achieve simplified post-processing, improved purity and yield, and mild reaction conditions Effect
CN108727207BActive Publication Date: 2021-03-05SHANGHAI INST OF PHARMA IND CO LTD +1
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Patent Information

Authority / Receiving Office
CN ยท China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND CO LTD
Publication Date
2021-03-05

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Abstract

The invention discloses a preparation method of an intermediate of a tyrosine kinase inhibitor. The preparation method of the intermediate of the tyrosine kinase inhibitor of the present invention comprises the following steps: in ethyl acetate and water, under the action of ammonium chloride and iron powder, compound II is subjected to the following reaction to obtain compound I. The method has high product yield and purity, simple post-treatment, and is suitable for industrial production:
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Description

technical field

[0001] The invention relates to a preparation method of an intermediate of a tyrosine kinase inhibitor. Background technique

[0002] tivozanib hydrochloride monohydrate (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor designed to treat Refractory Advanced RCC. It was discovered by Kirin Co., Ltd. of Japan, and its European and American markets are cooperated by AVEO Pharmaceuticals of the United States and Astellas Pharma of Japan develop. The vascular endothelial growth factor (VEGF) pathway plays an important role in angiogenesis, which is critical in cancer and is essential for angiogenesis, the formation of new blood vessels, for endothelial cell proliferation, migration and survival. There are currently five known VEGF ligands (A, B, C, D, PLGF) and three VEGF receptors (1, 2, and 3), and for optimal inhibition of the VEGF pathway, it is critical to effectively block all Three VEGF receptors, as they play an important role in cancer angioge...

Claims

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