190728-25-7Relevant academic research and scientific papers
Crystal structures of intermediates in a new synthesis of antitumor drug cabozantinib
Laus, Gerhard,Schreiner, Erwin,Nerdinger, Sven,Kahlenberg, Volker,Wurst, Klaus,Vergeiner, Stefan,Schottenberger, Herwig
, p. 323 - 332 (2016)
The heterocyclic antitumor drug cabozantinib was synthesized by condensation of 4-(6,7-dimethoxyquinolin-4-yloxy)aniline and methyl 1-(4-fluorophenylcarbamoyl)cyclopropanecarboxylate in the presence of two equivalents of sodium methoxide and azeotropic re
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors
Kettle, Jason G.,Anjum, Rana,Barry, Evan,Bhavsar, Deepa,Brown, Crystal,Boyd, Scott,Campbell, Andrew,Goldberg, Kristin,Grondine, Michael,Guichard, Sylvie,Hardy, Christopher J.,Hunt, Tom,Jones, Rhys D. O.,Li, Xiuwei,Moleva, Olga,Ogg, Derek,Overman, Ross C.,Packer, Martin J.,Pearson, Stuart,Schimpl, Marianne,Shao, Wenlin,Smith, Aaron,Smith, James M.,Stead, Darren,Stokes, Steve,Tucker, Michael,Ye, Yang
, p. 8797 - 8810 (2018)
While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to establish
Synthesis method of cabozantinib and intermediate thereof
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Paragraph 0113-0117, (2021/02/24)
The invention provides a synthesis method of cabozantinib and an intermediate thereof, and belongs to the field of medicinal chemistry. According to the invention, cyclopropane-1,1-dicarboxylic acid amine is used as a key intermediate, and reacts with sub
Preparation method of cabozantinib or salt thereof
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Paragraph 0036-0038; 0045-0046, (2021/06/22)
The invention relates to a preparation method of cabozantinib or a salt thereof, which comprises the following steps: taking a compound shown as a formula I and 1-((4-fluorophenyl)carbamoyl)cyclopropanecarboxylic acid as raw materials, conducting reacting
PAN-KIT KINASE INHIBITOR HAVING QUINOLINE STRUCTURE AND APPLICATION THEREOF
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Paragraph 0067-0068, (2021/10/22)
Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug
PYRIDONE COMPOUNDS AND METHODS OF USE IN THE MODULATION OF A PROTEIN KINASE
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Paragraph 0414-0415; 0417, (2021/04/02)
The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.
COMPOUNDS AND METHODS OF USE
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Paragraph 0205-0208; 0210, (2021/09/04)
The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.
COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
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, (2020/08/13)
The present invention relates to compounds that modulate cellular activities such as proliferation, differentiation, programmed cell death, migration, and chemoinvasion, by modulating protein kinase enzymatic activity, and compositions thereof, and methods of using such compounds.
Preparation method of cabozantinib defluorination impurity
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Paragraph 0019; 0035-0036, (2020/08/25)
The invention discloses a preparation method of a cabozantinib defluorination impurity. The method comprises the following steps: preparing an intermediate 1, preparing 4-chloro-6, 7-dimethoxyquinoline, preparing an intermediate 2, and removing fluorine i
Synthesis method of cabozantinib dimer
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Paragraph 0022-0023; 0030-0031, (2020/07/28)
The invention discloses a synthesis method of a cabozantinib dimer. The method comprises the following steps: preparation of 4-chloro-6,7-dimethoxyquinoline, preparation of an intermediate 1, and preparation of a cabozantinib dimer impurity; and preparati
