With four imidazopyridine-containing drugs and one pyrazolopyridine-containing drug on the market, bicyclic pyridines containing ring-junction nitrogen are privileged structures in medicinal chemistry. With two nitrogen atoms with potential to serve as hydrogen bond acceptors, imidazopyridines and pyrazolopyridines may boost binding to target proteins and elevate potency. In addition, these structures have found utility in FBDD, covalent inhibitors, reducing metabolic liabilities, and creating novel chemical space and intellectual properties. With many of the advanced intermediates now commercially available, they will find more and more applications in drug discovery.
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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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