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Click chemistry is an approach to chemical synthesis that emphasizes efficiency, simplicity, selectivity, and modularity in chemical processes used to join molecular building blocks. It includes both the development and use of "click reactions", a set of simple, biocompatible chemical reactions that meet specific criteria like high yield, fast reaction rates, and minimal byproducts. It was first fully described by K. Barry Sharpless, Hartmuth C. Kolb, and M. G. Finn of The Scripps Research Institute in 2001.[1][2] In this seminal paper, Sharpless argued that synthetic chemistry could emulate the way nature constructs complex molecules, using efficient reactions to join together simple, non-toxic building blocks.
The term "click chemistry" was coined in 1998 by Sharpless' wife, Jan Dueser,[3] who found the simplicity of this approach to chemical synthesis akin to clicking together Lego blocks. In fact, the simplicity of click chemistry represented a paradigm shift in synthetic chemistry, and has had significant impact in many industries, especially pharmaceutical development. In 2022, the Nobel Prize in Chemistry was jointly awarded to Carolyn R. Bertozzi, Morten P. Meldal and Sharpless, "for the development of click chemistry and bioorthogonal chemistry".[4]