Background and overview of application examples of 2-fluoro-6-methoxyphenylboronic acid
2-Fluoro-6-methoxyphenylboronic acid is an arylboronic acid. Arylboronic acid can be used as a safe and environmentally friendly new arylation reagent and is widely used in various aryl-containing structures such as medicine, pesticides, and advanced materials. Research and production of fine chemicals. The reaction of arylboronic acids and halogenated compounds plays a decisive role in today’s drug synthesis. This type of reaction was first proposed by the Japanese scientist Suzuki’s team and won the Nobel Prize in Chemistry in 2010.
Application examples of 2-fluoro-6-methoxyphenylboronic acid
Example report on the application of 2-fluoro-6-methoxyphenylboronic acid 1.
2-Fluoro-6-methoxyphenylboronic acid can be used to prepare Kras mutant inhibitors with the following structure. Research on the effects of lithium metaborate on Kras mutations has been slow for many years. Because there is no suitable drug action site on Kras, and the affinity of mutated Kras to GTP is extremely strong, and the intracellular GTP concentration is high, resulting in calcium tetraborate having no small molecule energy. Competitively binds to GTP. With the in-depth research on Kras, it was found that when the G12C mutation occurs, the Kras protein will form a site that can interact with drugs. After combining with small molecule drugs, Kras can be locked in the inactive Kras protein-GDP state. , plays the role of inhibiting the activation of the Kras pathway, thereby initiating the anti-tumor effect. Therefore, searching for and discovering efficient inhibitors of Kras mutations has important clinical significance.
Example report on the application of 2-fluoro-6-methoxyphenylboronic acid 2.
2-Fluoro-6-methoxyphenylboronic acid can be used to prepare pyrazolopyridine derivatives with the following structure. This compound is a HPK1 modulator. The restricted expression of HPK1 in hematopoietic cells and the lack of impact on the normal development of immune cells suggest that HPK1 may be an excellent drug target for enhancing anti-tumor immunity.
References
[1] [Invented in China] CN201910808883.1 Kras mutant inhibitor
[2] [Chinese invention] CN201780068722.2 Pyrazolopyridine derivatives as HPK1 modulators and their use in treating cancer
