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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Oxygen heterocycles are one of the most common heterocycles in drugs and natural products. Oxetene has high polarity and is also a good acceptor for hydrogen bond, which contributes to the metabolism and chemical stability of its host molecules. When substituted for commonly used functional groups such as gem dimethyl or carbonyl, oxetane units can induce profound changes in water solubility, lipophilicity, metabolic stability and conformational preference. Four of the FDA-approved drugs contain oxetenes: Orlistat, Paclitaxel, and two of its derivatives, Docetaxel and Cabazitaxel. Currently, oxetane-containing building blocks are flourishing in medicinal chemistry and drug discovery.
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