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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Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
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