54901-09-6Relevant academic research and scientific papers
Pyrazole derivative for FGFR inhibitor and preparation method of pyrazole derivative
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Paragraph 0214-0216, (2021/03/06)
The invention provides a pyrazole derivative for an FGFR inhibitor and a preparation method of the pyrazole derivative. The invention specifically relates to an amide pyrazole compound serving as an FGFR irreversible inhibitor, and a preparation method and application thereof. The present invention provides a compound as shown in Formula I, or a pharmaceutically acceptable salt, or solvate, isotope substitute, prodrug, or metabolite thereof. The compound as shown in general formula I have FGFR inhibitory activity, and is capable of preventing or treating disorders associated with FGFR activityor expression, preferably such as cancer.
Asymmetric total synthesis of dihydroisocoumarins: 6-methoxymellein, kigelin and fusarentin 6, 7 dimethyl ether by employing proline catalysed asymmetric α-aminoxylation
Mane, Baliram B.,Markad, Sachin B.,Waghmode, Suresh B.
, (2020/10/19)
A concise asymmetric total synthesis of dihydroisocoumarins such as 6-methoxymellein, kigelin and fusarentin 6,7-dimethyl ether in high enantiopurity have been achieved from non-chiral aldehydes by employing proline catalysed asymmetric α-aminoxylation reaction. The required stereochemistry of hydroxyl group have been generated by alternating L or D proline as a organocatalyst in α-aminoxylation step and lactone ring is assembled by oxa-Pictet-Spengler cyclisation reaction as the key steps.
Vinyl sulfamido substituted pyrazolyl benzamide compound
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Paragraph 0093-0094, (2020/07/02)
The invention provides a vinyl sulfamide substituted pyrazolyl benzamide compound. Specifically, the present invention provides a compound in formula I shown in the specification or a pharmaceuticallyacceptable salt thereof, and a preparation method and use thereof. The compound shown in the formula I has excellent FGFR inhibitory activity and can be used for preventing or treating diseases related to FGFR kinase activity or expression quantity, such as cancer.
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors
Fan, Jun,Dai, Yang,Shao, Jingwei,Peng, Xia,Wang, Chen,Cao, Sufen,Zhao, Bin,Ai, Jing,Geng, Meiyu,Duan, Wenhu
, p. 2594 - 2599 (2016/05/09)
Fibroblast growth factor receptors (FGFRs) are important oncology targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. We identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound 29 strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that 29 was a potent pan-FGFR inhibitor. The flexibility of our structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy.
A convenient and effective synthesis of 3-(3,5-dimethoxyphenyl)propanal
Nikas, Spyros P.,Thakur, Ganesh A.,Makriyannis, Alexandros
, p. 1751 - 1756 (2007/10/03)
A convenient and effective synthesis of 3-(3,5-dimethoxyphenyl) propanal, an important intermediate in the synthesis of various biologically active compounds is described.
