Click Chemistry and Pharmaceutical Manufacturing


On 5 October 2022, the Royal Swedish Academy of Sciences announced that Barry Sharpless, Caroline Bertuzzi, and Morten Meldal were awarded the Nobel Prize in Chemistry; for their contribution to establish a new methodology for the formation of complex compounds, called "click chemistry".

Chemist Barry Sharpless is one of the few scientists to win the Nobel Prize twice. In the year he was awarded his first Nobel Prize, his paper on click chemistry was published. He was the first to introduce this term, which means inducing chemical reactions to link chemical building blocks that efficiently results in new materials under simple and appropriate conditions.

It is similar to snapping Lego blocks together; if we want to build any shape, we will use the appropriate cubes, and the output will be the shape we first planned. Similarly, the outputs of click reactions are chemicals produced without any secondary products that are difficult to separate. Click reactions are rapid and easily prepared; they can occur at room temperature in both air and water, the products are easily separated, and obtaining huge quantities of products is possible.

The interactions of click chemistry have different forms; the most famous is the copper-catalyzed azide-alkyne cycloaddition that Barry Sharpless and Morten Meldal discovered independently. Azides are compounds that contain three nitrogens bonded together, and alkynes are hydrocarbons that contain carbon-carbon triple bonds. However, to create interactions within living organisms, the copper catalyst cannot be used due to its toxicity. Caroline Bertozi devised a method for removing the copper catalyst, called the bioorthogonal reactions.

These reactions are rapid and take only a few minutes to occur. This reduces the side effects, and does not disrupt the biochemical processes. Pharmaceutical applications of bioorthogonal chemistry include: the development of cancer drugs targeting cancer cells only, labeling biomolecules with fluorescent dye for tracking the drug, diagnosis, or studying the tissue, biomolecules or drug reactions.

The advantages of click chemistry in synthesizing compounds easily with high-efficient methods that have never been obtained before. Click and bioorthogonal chemistry will open the door for researchers to innovate in the fields of pharmacological discovery and drug development, and this will benefit all humanity.


Cover Image: Illustration: ©Johan Jarnestad/The Royal Swedish Academy of Sciences. Source:

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