A team of chemists at Scripps Research and Rice University has devised a groundbreaking method to synthesize complex, three-dimensional molecules known as piperidines, which are crucial components in many pharmaceuticals. This innovative approach combines biocatalytic carbon-hydrogen oxidation and radical cross-coupling, offering a streamlined and cost-effective alternative to traditional methods. The discovery has the potential to accelerate drug discovery and advance the field of medicinal chemistry.
A team of chemists from Scripps Research and Rice University has developed a novel method to simplify the synthesis of piperidines, a key structural component in many pharmaceuticals. The study, published in Science , 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 .
Modern medicinal chemists face increasing challenges as they target complex molecules to address difficult biological targets. Traditional methods for synthesizing flat, two-dimensional molecules, such as pyridines, are well established, but strategies for their 3D counterparts, like piperidines, have been far more elusive. 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. In the second step, these newly functionalized piperidines undergo radical cross-coupling with nickel electrocatalysis. This approach forms new carbon-carbon bonds efficiently by connecting different molecular fragments without the need for extra steps, like adding protective groups that shield parts of the molecule during synthesis or using expensive precious metal catalysts such as palladium. This two-step process dramatically simplifies how complex piperidines are built. We have essentially created a modular approach to simplify piperidine synthesis, analogous to how palladium cross-coupling revolutionized pyridine chemistry decades ag
Piperidine Synthesis Drug Discovery Medicinal Chemistry Biocatalysis Radical Cross-Coupling
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