The traditional process of drug discovery based on natural secondary metabolites has often been slow, costly, and labor-intensive. Even with the advent of combinatorial chemistry and high-throughput screening in past decades, the generation of leads is dependent on the reliability of the individual reactions to construct the new molecular framework.
Click chemistry is a newer approach to the synthesis of drug-like molecules that can accelerate the drug discovery process by utilizing a few practical and reliable reactions. Sharpless and coworkers defined what makes a click reaction as one that is wide in scope and easy to perform, uses only readily available reagents, and is insensitive to oxygen and water. In fact, in several instances, water is the ideal reaction solvent, providing the best yields and highest rates. Reaction work-up and purification uses benign solvents and avoids chromatography.1
Click chemistry involves the use of a modular approach and has important applications in the fields of drug discovery, combinatorial chemistry, target-templated in situ chemistry, and DNA research.1
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