Unlocking ketones

Methylene groups, a ubiquitous structural feature of small molecule therapeutics, are notoriously nonreactive. This makes it challenging to modify them, a process vital to generating drug derivatives and new drug scaffolds.

Researchers at the University of Illinois at Urbana-Champaign (UIUC) think they have solved the problem. They have developed a chemical reaction that selectively oxidizes methylene groups and turns them into much more reactive ketones that can be converted to a wide range of other functional groups such as alcohols, ethers and esters.¹The technique could open new chemical space by allowing natural products and other structures to be oxidized at carbon sites that were previously difficult or impossible to modify with traditional medicinal chemistry techniques...