Halogenated Heterocycles for Drug Discovery

Abstract

Within a number of industries, and particularly within the pharmaceutical industry, there is a desire for reliable, high yielding routes towards large numbers of valuable small molecules that allow a wide range of products to be synthesised.

Heterocyclic compounds are particularly sought after as useful compounds, with an estimated 70% of pharmaceutical products being based on heterocyclic structures. A drawback of many traditional routes towards heterocyclic compounds is that the range of substituents that may be placed around the ring is limited. This is especially limiting if ring substituents have to be placed early in a synthesis, reducing the opportunities for elaboration at a late stage.

Our approach is to take highly halogenated heterocyclic systems and use them as scaffolds for the synthesis of novel compounds by the sequential replacement of halogen atoms with other functionalities.

This approach has led to the generation of a number of novel highly substituted heterocyclic species.