EPSRC grant for Prof Iain Coldham

Prof Iain Coldham has been awarded funding from the Engineering and Physical Sciences Research Council (EPSRC) for a project entitled "C-H functionalisation of saturated nitrogen heterocycles, building blocks for drug discovery". The project aims to develop synthetic chemistry and an understanding of the methodology to give substituted nitrogen-containing heterocycles of relevance to the pharmaceutical industry.

The project is a collaboration with theoretical chemist Prof Anthony Meijer, who will provide input through DFT calculations on the structures and barriers to interconversion of the compounds. In addition, it involves a collaboration with the company Liverpool ChiroChem, who will provide a steer for the industrial relevance of the chemistry with the aim to provide compounds of value as scaffolds for drug synthesis.

Current methods to prepare even fairly simple multi-substituted, saturated nitrogen-containing ring systems that are of medicinal relevance are often long-winded and complex, particularly for quaternary substituted compounds where more than one substituent is located on the same carbon atom. This project will use simple chemistry with readily available reagents to prepare novel substituted heterocycles, including quaternary substituted compounds. The chemistry uses a simple deprotonation, yet this provides a powerful way to provide a range of different products and allows the ability to control the absolute configuration to prepare heterocycles that are enriched as a single mirror image. As an example of the type of chemistry, see this recent article in Chemical Science and the general scheme shown here.

Chrial ligand mechanism

This work is supported by EPSRC grant: EP/R024294/1