Due to a breakthrough in mechanistic understanding, researchers at the University of Manchester have developed the first example of a ruthenium-catalyst capable of near room temperature late-stage C-H functionalisation, vastly outperforming all other catalysts in the market.
Over the last decade, synthetic techniques that allow the late-stage functionalisation (LSF) of biologically active molecules have been of great interest for accelerating drug development and, for their ability to access structures that would be too challenging or time consuming to make otherwise.
LSF reactions are commonly catalysed by platinum or palladium catalysts which are expensive to use and have limited solvent tolerances. Ruthenium catalysts are also used to catalyse LSF reactions but, are often overlooked due to their poor catalytic activity.
The University of Manchester’s new class of Ru catalysts exhibit very high reactivity and are suitable
for C-H functionalisation reactions of arenes with a N-containing directing group. They can directly functionalise ‘real’ biologically relevant molecules where current catalysts fail.
Our catalysts are so powerful that such transformations can be performed at close to room temperature and display spectacular functional group compatibility. Furthermore, our catalyst is exceptionally soluble in most organic solvents as well as in water, which opens-up applicability to other reactivities.
Considering their unique and unprecedented efficacy, our catalysts can be used to C-H arylate and/or alkylate complex molecules allowing chemo selective functionalisation of complex drugs in high yields.
Benefits and Impact:
Our catalysts enable a facile route to otherwise complex synthetic pathways which will reduce drug discovery and development cycle times for the pharmaceutical industry.
Our catalyst is:
- Air stable, heterogenous catalysts.
- High yielding, low cost and easy to produce at scale.
- Lower cost than equivalent Pd-catalysts.
- Very low catalyst loadings required (as low as 0.25 mol %).
- Exceptional solubility-functionalisation can be carried out in vast array of organic solvents, including green solvents.
Target Markets and Applications:
We anticipate that our new class of ruthenium catalyst will be beneficial to pharmaceutical research and development for the acceleration of drug discovery.
