Synthesis method of pyrotinib

A technology of pyrotinib and synthetic method, applied in the field of pharmaceutical chemical synthesis, can solve the problems of high cost, easy oxidation and deterioration, low industrial production value and significance
CN112110899AActive Publication Date: 2020-12-22SUZHOU FUSHILAI PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUZHOU FUSHILAI PHARMA CO LTD
Publication Date
2020-12-22

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Abstract

The invention discloses a synthesis method of pyrotinib, which belongs to the technical field of chemical synthesis of medicines. The preparation method comprises the following steps of firstly, reacting 2-[(4-bromo-2-chlorophenoxy)methyl]pyridine with n-butyllithium at a low temperature, and then carrying out a boronation reaction with an organic boron reagent to obtain [3-chloro-4-(pyridine-2-ylmethoxy)phenyl]boric acid, enabling (2E)-N-(4-amino-3-cyano-7-ethoxy quinoline-6-yl)-3-[(2R)-1-methyl pyrrolidine-2-yl] acrylamide and the obtained [3-chloro-4-(pyridine-2-yl methoxy)phenyl]boric acid to be subjected to a catalytic coupling reaction in a system of a copper catalyst, a base catalyst and a solvent, and acquiring pyrotinib. The method has the characteristics of readily available rawmaterials, simple process, economy, environmental protection and the like, is beneficial to quality control and improvement of final product raw material medicines, is suitable for industrial production and is beneficial to promoting cheap development of the raw material medicines.
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Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical chemical synthesis, and in particular relates to a synthetic method of pyrotinib. Background technique

[0002] Pyrotinib is an irreversible human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) dual-target tyrosine kinase inhibitor independently developed by China Jiangsu Hengrui Pharmaceutical Company The mechanism of action is to covalently bind to the adenosine triphosphate (ATP) binding site of the HER2 and EGFR kinase domain in the cell, prevent the formation of homogeneous and heterogeneous dimers of HER2 and EGFR in tumor cells, and inhibit its own phosphorylation, Block the activation of downstream signaling pathways, thereby inhibiting tumor cell growth. Pyrrotinib maleate tablets were officially approved by the China Food and Drug Administration (CFDA) in August 2018 for the treatment of epidermal growth factor receptor 2 (HER2) positive pat...

Claims

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