Imidazole is an important five-membered nitrogen-containing heterocyclic compound. Among the numerous heterocyclic compounds, imidazole and its derivatives are regarded as a unique and multifaceted scaffold material due to their diverse applications in industrial, organic and pharmaceutical chemistry. Imidazoles interact in different ways with many therapeutic targets, enzymes and receptors in biological systems and thus exhibit a wide range of biological activities. In particular, several imidazoles can be used as clinical drugs to treat various types of cancer with high therapeutic efficacy. Furthermore, imidazoles are one of the most critical segments in the field of anti-covid-19 virus drug discovery due to their ability to interact with active targets in living systems.
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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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