A team of chemists has unveiled a novel method to simplify the synthesis of piperidines, a key structural component in many pharmaceuticals. The study combines biocatalytic carbon-hydrogen oxidation and radical cross-coupling, offering a streamlined and cost-effective approach to create complex, three-dimensional molecules.
This innovation could help accelerate drug discovery and enhance the efficiency of medicinal chemistry.
To bridge this gap, the team introduced a two-stage process to modify piperidines, which are important in many pharmaceuticals. The first step uses biocatalytic carbon-hydrogen oxidation, a method where enzymes selectively add a hydroxyl group to specific sites on piperidine molecules. This process is similar to a common chemical technique called electrophilic aromatic substitution, which works for flat molecules like pyridines, but here it is applied in a 3D structure.
The research demonstrated the streamlined synthesis of numerous high-value piperidines used in natural products and pharmaceuticals, including neurokinin receptor antagonists, anticancer agents and antibiotics. The approach reduced multistep processes from 7-17 steps to just 2-5, drastically improving efficiency and cost.
"By combining biocatalytic oxidation and radical cross-coupling, we are enabling access to molecules previously considered inaccessible or prohibitively expensive," said Yu Kawamata, a co-author and institute investigator in the Department of Chemistry at Scripps Research. Financial support for this work was provided by National Institutes of Health , the Welch Foundation , fellowship support from the Naito Foundation and NSF REU grant 2150216.Chicago
Pharmaceuticals Today's Healthcare Controlled Substances Organic Chemistry Chemistry Biochemistry Inorganic Chemistry
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