The creation of new molecular entities and subsequent exploitation of their properties is central to a broad spectrum of research disciplines from medicine to materials but progress has been limited by the difficulties associated with chemical synthesis. There are many tools available in synthesis and we have focused on exploiting the chemistry of boron to facilitate this endeavour. Boron is an unusual element in that it is normally has three groups around it but this makes it vulnerable to attack by a fourth group since most elements (e.g. carbon) like to have 4 groups around them However, once it has 4 groups it readily expels one of them to go back to three groups – its behaviour makes it rather schizophrenic. This feature is exploited in a fundamentally new strategy, which has the potential to revolutionise how we conduct complex organic synthesis. By adding a fourth group that has an adjacent leaving group attached, one of the three groups on boron migrates expelling the leaving group creating a new C–C bond. C–C bond formation is fundamental to organic synthesis. In so doing, it generates a new organo-boron compound which can react again and again multiple times making complex organic synthesis easier than before.
To realise this strategy, we need to develop new ways of introducing boron into molecules (introductory phase), a family of reagents which react with the organoboron compound effecting chain growth (growth phase), and new methods to transform the carbon-boron bond into other functional groups (termination phase). This will enable complex molecules to be made more easily.
In addition we seek to use the precise control of stereochemistry that this methodology enables to create molecules with tailored shape, be they helical or linear. By doing this we will be able to create molecules with substituents hanging from the main chain at precise positions and they will be used to dock and disrupt certain protein-protein interactions involved in cancers.
The methodology is also being used to target natural products which are members of the polyketide family since many of them have profound anti-bacterial/anti-inflammatory and anti-cancer properties.
