Background and overview of application examples of 2-hydroxy-5-pyrimidineboronic acid
2-Hydroxy-bromopyridine-5-pyrimidineboronic acid is a pharmaceutical intermediate that can be used for Suzuki and other coupling reactions. There are reports in the literature that it can be used to prepare drugs for treating AIDS, kinase inhibitors and EIF4E inhibitors.
Application examples of 2-hydroxy-5-pyrimidineboronic acid
Example report on the application of 2-hydroxy-5-pyrimidineboronic acid 1.
CN201180038442.X reported that 2-hydroxy-5-pyrimidineboronic acid can be used to prepare naphthyl-2-yl acetic acid derivatives with the following structure. The medicament is used to treat (eg prevent, modulate or inhibit) the HIV virus or AIDS or to delay the onset of symptoms of AIDS or ARC in a mammal (eg a human). Human immunodeficiency virus (HIV) infection and related diseases are major public health problems worldwide.
Example report on the application of 2-hydroxy-5-pyrimidineboronic acid 2.
2-Hydroxy-5-pyrimidineboronic acid can be used to prepare kinase inhibitors with the following bicyclic heteroaryl groups. This class of compounds has inhibitory effects on kinases including LRRK2, DLK, MLK1, MLK2 and MLK3. Mammalian protein kinases are involved in the regulation of important cellular functions. Protein kinases are targets for drug development due to the fact that dysfunction of protein kinase activity is associated with several diseases and conditions. Mixed lineage kinases (MLKs) are MAPK kinase kinases that target JNK and p38 MAPK for activation in response to different stimuli in stressed cells.
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Example report on the application of 2-hydroxy-5-pyrimidineboronic acid 3.
2-Hydroxy-5-pyrimidineboronic acid can be used to prepare benzoic acid derivatives with the following structure as EIF4E inhibitors. Eukaryotic initiation factor 4E (eIF4E) is a 24kDa protein that plays an important role in initiating the translation of mRNA. During the initiation of mRNA translation, eIF4E binds to the 7-methylguanine nucleoside cap structure at the 5′ end of the mRNA and forms a complex (called eIF4F) with the scaffold protein picolin eIF4G and the helicase eIF4A. Formation of this complex is required to initiate cap-dependent translation, and therefore binding of eIF4E to eIF4G is a key event in this process. eIF4E has been identified as a promising target in the field of oncology due to the large body of data implicating it in transformation and tumorigenesis.
References
[1][Invented in China] CN201180038442.X naphthalene-2-yl acetic acid derivatives for treating AIDS
[2][China invention, China invention authorization] CN201180036376.2 bicyclic heteroaryl kinase inhibitor and method of use
[3][China invention, China invention authorization] CN201280057180.6 Benzoic acid derivatives as EIF4E inhibitors
