Chemists at the Ohio State University developed a new way to synthesize carbenes, essential components of drug synthesis and materials development. They published their findings in Science.
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Their new method works by using iron as a metal catalyst with dichloride compounds that easily generate free radicals. These substrates form carbenes with various substituents. Then, the carbenes bond with another molecule to form a triangular cyclopropane, which is vital in the synthesis of medicine and agrichemicals.
Saving time and money
Carbenes are reactive carbon molecules with an unbonded electron pair. They act as intermediates in many reactions, but their precursors are unstable and hazardous. The new method involves dichloride compounds, an iron catalyst and a zinc reductant, all of which are relatively stable. The new technique can also generate various carbenes with different substituents bonded to the central carbon.
The traditional method of carbene synthesis involves a wasteful multi-step reaction. Future drugs synthesized by this more efficient method could be cheaper for consumers. The new method could also prevent medicine shortages, according to David Nagib, co-author of the study and a professor of chemistry and biochemistry at The Ohio State University.
This method could also make drugs that are cheaper, more potent, faster-acting and longer-lasting.
“Our lab is obsessed with trying to get the best methods for making cyclopropanes out there as soon as possible,” said Nagib, “We have the eye on the prize of inventing better tools to make better medicines, and along the way, we’ve solved a huge problem in the carbene world.”
Water-compatible carbenes open the door to in-cell drug chemistry
The researchers found that this method also works well in water, indicating that carbenes may be able to be synthesized inside a living cell, which could enable the discovery of new drug targets.
The team is dedicated to ensuring that this improvement is accessible to research labs and drug manufacturers globally. To this end, they are continuing to improve the process, said Nagib.
This work was supported by the National Science Foundation, the National Institutes of Health and the Brown Institute for Basic Science.
