Indazoles are a class of organic heterocyclic compounds, also known as 1,2-diazaindene and benzopyrazole. Indazole is a good bioisomer of phenol, which is more lipophilic than phenol and less prone to phase I and II metabolism. Indazole derivatives have a wide range of biological activities, and it has been confirmed that indazole compounds have anti-tumor, analgesic, anti-inflammatory and other drug activities. Anticancer is the most important application field of indazole drugs. Renal cell carcinoma, solid tumor, nausea and vomiting caused by chemotherapy and leukemia are the main indications of this structural backbone drug.
Boronic acids and boronate esters are commonly used reagents in Suzuki–Miyaura coupling chemistry. Organoboron derivatives are common reagents for C–C bond formation, either through classical palladium-mediated transformations or through other newer coupling methods. Boronic esters and acids are potential intermediates in the manufacture of many active pharmaceutical ingredients (API).
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Fluorine is the most electronegative element in the periodic table, and the fluorine atom has a small atomic radius, so fluorine-containing organic compounds have many wonderful properties. For example, the introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the permeability to cell membranes, metabolic stability and bioavailability; in addition, the introduction of fluorine atoms will improve the lipid solubility of the compound and promote its absorption in the body. The speed of delivery changes the physiological effect. In the field of medicinal chemistry, the introduction of fluorine atoms into organic molecules is an important direction for the development of new anticancer drugs, antitumor drugs, antiviral agents, anti-inflammatory drugs, and central nervous system drugs.
Tetrahydropyran is an organic compound consisting of a saturated six-membered ring containing five carbon atoms and one oxygen atom. Tetrahydropyrans are common structural motifs in natural products and synthetic therapeutic molecules. In nature, these six-membered oxygen heterocycles are usually assembled by intramolecular reactions, including oxygen Michael addition or ring opening of epoxy alcohols. In fact, polyether natural products have been particularly extensively studied for their fascinating structures and important biological properties; these are often formed through endoselective epoxy open cascades.