Cross-Coupling Reactions Leading to Chiral Heterocyclic Scaffolds for Drug Development and Manufacturing

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Heterocycles, cyclic molecules with at least one non-carbon atom, are widely used in drug discovery and development due to their favourable physical and chemical properties. Pyridines are the most widely used aromatic heterocycle in FDA approved drugs and there is a continued demand for methods to prepare them and their derivatives. Unfortunately, the majority of methods to do this employ harsh reaction conditions and are therefore not widely useful. We have devised a conceptually new approach to make pyridine derivatives using exceptionally mild conditions that tolerate a wide range of functional groups. These reactions also provide immediate access to small molecules that possess 'drug-like' qualities and that are hard to make by other means. Finally, our methods are catalytic and therefore will contribute to the reduction of the environmental costs of drug discovery and development. As a result, the proposed research will have a direct impact on the search for new therapeutic agents.