Researchers at the Korea Advanced Institute of Science and Technology have developed a groundbreaking technique that allows them to replace an oxygen atom with a nitrogen atom in a molecule. This process, known as photocatalysis, could pave the way for more efficient drug development by enabling targeted changes to the structure of complex molecules. The team’s findings, published in the journal Science, suggest this ‘pencil-and-eraser’ approach could revolutionize how chemists approach molecular engineering.
Shining Light on Molecules
A little use of light enables great development: Chemists have essentially promoted the replacement of an oxygen atom with a nitrogen atom in the mechanosynthesis (i.e., chemical synthesis during grinding) of compounds. The ‘pencil-and-eraser’ method, which its developers have dubbed, is detailed in the journal Science and promises to expand the toolkit available for chemists looking to rapidly alter the structure of complex molecules.
All such attempts made to alter molecular structure at atomic scales have suffered from a number of problems, primarily including the delocalisation of electrons and applied under extreme conditions (high temperatures or radiation). Nevertheless, the Korean researchers from the Korea Advanced Intsistute of Science and Technology managed to circumvent these issues using a photocatalytic strategy. Light initiates a cascade of electron and proton transfers that replace an oxygen atom in a furan ring with a nitrogen one.
Opening Doors for Drug Development
The impact of this finding is great, in particular for drug development. As Ellie Plachinski and Tehshik Yoon from the University of Wisconsin-Madison note in an article published in Science about the study, small tweaks to a molecule can change its usefulness as a drug.
Until now, when chemists have wanted to make small changes—like swapping out a single atom—they had to synthesize molecules from scratch. This has relegated the process as tedious sometimes- a pace which curbs their ability to exploit complex molecules in all its complexity. Still, Korean research team’s new photocatalytic method not only allows for more precise molecular editing in less steps but also introduces novel strategies toward drug discovery and development.
Influenced by Previous Successes
The groundbreaking work was inspired by a study published in 1971 by chemists Axel Couture and Alain Lablache-Combier. In experiments for their research they used ultraviolet light to transform a furan molecule into an N-propylpyrrole, showing that the photochemistry has potential benefits for modifying molecular structures.
Taking the work one step further, the Korean team has since developed a more general method to carry out efficient and selective oxygen-to-nitrogen replacements using photocatalysis. This major event demonstrates the value of science teamwork, and how a country can benefit by combining basic research with practice to encourage chemistry progress.
