848139-78-6Relevant articles and documents
Synthesis method of pyrrotinib maleate intermediate
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, (2021/09/04)
The invention relates to the technical field of medicine synthesis, in particular to a synthesis method of a pyrrotinib maleate intermediate. The synthesis method comprises the following steps: by taking a formula II as an initial raw material, reacting the formula II with cyanoacetamide under the action of a sulfonic acid compound to obtain a compound shown in a formula III; carrying out heating reflux reaction on the compound as shown in the formula III, 4-nitro-3-ethoxyaniline and triethyl orthoformate, and obtaining a solid intermediate product after the reaction is finished; subjecting the obtained solid intermediate product and Lewis acid to a heating ring closing reaction to obtain a compound shown in a formula IV; and carrying out reduction reaction on the compound as shown in the formula IV, hydrazine hydrate and activated carbon under the action of a catalyst to prepare the compound as shown in the formula I, namely the pyrrotinib maleate intermediate disclosed by the invention. The method is short in reaction route, high in yield, simple and convenient to operate, free of extreme reaction conditions and expensive raw materials, lower in production cost and beneficial to industrial production.
Preparation Method for Tyrosine Kinase Inhibitor and Intermediate Thereof
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Paragraph 0090, (2020/08/19)
Provided is a preparation method for a tyrosine kinase inhibitor and an intermediate thereof. Specifically, a preparation method for a cyanoquinoline compound is provided. The method has a high yield, good product purity, and mild reaction conditions.
Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro
Jin, Shuyu,Sun, Xiuyun,Liu, Dan,Xie, Hua,Rao, Yu
, p. 1333 - 1345 (2019/05/06)
The discovery and development of a novel HER-2 tyrosine kinase inhibitor for the treatment of HER2-positive breast cancer are presented in this article. EGFR family has been recognized as a crucial meditator in the cancer progression; HER-2 tyrosine kinase was one of the members among them. In the effort to explore potent HER-2 inhibitors, a novel series of 4-anilino-3-cyanoquinoline derivatives have been designed, synthesized and evaluated. Most compounds possessed modest proliferation inhibition on SK-BR-3 cell line and HER-2 kinase. Compound 16 appeared to be the most potent compound (HER-2 kinase IC50: 19.4?nM, SK-BR-3 IC50: 94?nM). In the experiment of cellular cytotoxicity assay, compound 16 shows a much lower cytotoxicity than neratinib on Beas-2b cell line (Human bronchial epithelial cells). In conclusion, compound 16 would be a promising lead compound for further anti-breast cancer drug discovery.