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Researchers harness the energy of carbenes to fabricate drugs easier and much more safely

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Despite being probably the most versatile blocks in organic chemistry, compounds called carbenes could be too hot to take care of. In the lab, chemists often stay away from these highly reactive molecules because of how explosive they could be.

Yet in a fresh study, published today in the journal Science, researchers from The Ohio State University report on a fresh, safer solution to turn these short-lived, high-energy molecules to a lot more stable ones.

“Carbenes have an unbelievable level of energy inside them,” said David Nagib, co-author of the analysis and a professor of chemistry and biochemistry at Ohio State. “The worthiness of this is they are able to do chemistry which you cannot do any way.”

Actually, members of the Nagib Lab focus on harnessing reagents with such high chemical energy, and also have helped invent a variety of new substances and techniques that could otherwise be chemically unobtainable.

In this study, the researchers developed catalysts crafted from cheap, Earth-abundant metals, like iron, copper and cobalt, and combined them to facilitate their new approach to harnessing carbene.

These were in a position to successfully utilize this new technique to channel the energy of reactive carbenes to fabricate valuable molecules on a more substantial scale plus much more quickly than traditional methods. Nagib compared this leap to engineers determining how exactly to use steel to create skyscrapers instead of offline.

For example, one molecular feature that chemists have already been hard-pressed to generate is cyclopropane, a little, strained ring of twisted chemical bonds within some medicines. Recently, cyclopropane has been used as an integral ingredient in the oral antiviral pill called Paxlovid. Used to take care of COVID-19, the pill reduces the severe nature of the condition by stopping the herpes virus from replicating, instead of killing it outright.

Even though cyclopropane had a need to fabricate the drug has been difficult to generate in large quantities, Nagib said he believes his lab’s new method could possibly be put on create the drug quicker and at a more substantial scale. “Our new method will enable better usage of dozens of forms of cyclopropanes for incorporation into all sorts of medicines to take care of disease,” he said.

As the team’s research has potential applications beyond your pharmaceutical realm, like agrochemicals, Nagib said he’s most passionate about how exactly their tool could increase the discovery of new, targeted medicines. “You can technically apply our solutions to anything,” he said. “However in our lab, we’re interested in accessing new forms of stronger drugs.”

Nagib predicts that utilizing the process his team developed, a chemical reagent that currently takes 10 or 12 making (by explosive intermediates) could possibly be done in 4 or 5, knocking off nearly 75% of that time period it requires to fabricate.

Overall, Nagib said he hopes this research can help other chemists do their work.

“There are several excellent scientists all over the world who do that sort of chemistry and using our tool they might potentially have a safer lab,” Nagib said. “The flavor of science that people do, probably the most satisfying reward is when other folks use our chemical solutions to make important better.”

Other co-authors were Lumin Zhang, a former postdoctoral fellow, along with Bethany M. DeMuynck, Alyson N. Paneque and Joy E. Rutherford, all graduate students in the department of chemistry and biochemistry and members of the Nagib Lab.

More info: Lumin Zhang et al, Carbene reactivity from alkyl and aryl aldehydes, Science (2022). DOI: 10.1126/science.abo6443

Citation: Researchers harness the energy of carbenes to fabricate drugs easier and much more safely (2022, August 4) retrieved 4 August 2022 from

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