Bosutinib compound

Abstract

Belonging to the technical field of medicine, the invention in particular relates to a bosutinib monohydrate and a preparation method thereof. The bosutinib monohydrate obtained by the invention contains a crystal water, and has the advantages of: good stability, easy industrialized preparation process, good quality reproducibility, and well controlled product purity. The invention also relates to application of compositions using the hydrate in drugs treating chronic myeloid leukemia.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to bosutinib monohydrate and a preparation method thereof. The present invention also relates to the application of the hydrate composition in medicine for treating chronic myelogenous leukemia. Background technique [0002] Bosutinib is a potent protein kinase (Src-Abl) inhibitor, which can not only inhibit the autophosphorylation of Src protein in a variety of human tumor cells, but also inhibit the phosphorylation of Src and Abl substrates process. The drug was developed by Wyeth Pharmaceuticals, a subsidiary of Pfizer in the United States, and was first launched in the United States in September 2012. It is approved for chronic phase, accelerated phase or blast phase that is resistant or intolerant to previous treatment The treatment of adult patients with Philadelphia chromosome-positive chronic myelogenous leukemia (CML), the product name is Bosulif, and the spe...

AI Technical Summary

Problems solved by technology

However, the monohydrate crystal form obtained above has the following problems in the production process: (1) the yield is low, and it is difficult to realize in industrial production; (2) it is difficult to effectively improve the product purity, and it is difficult for a single impurity to reach 0.1% Below, and poor quality reproducibility during repetition

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