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Development of new Non-Toxic Methodology for the Synthesis of Important Pharmaceuticals Using Free Radicals

Objective



Research objectives and content

The application of the vast array of excellent synthetic procedures using triorganotin hydrides to pharmaceutical synthesis is precluded by the toxicity of organ tin. An increasing number of synthetic processes in thepharmaceutical industry use tributyltin hydride because the alternative methodology is lengthy, time consuming and costly. In these syntheses the removal of the toxic organotin residues to required non-toxic levels is also costly and time consuming. The essence of our project is to replace triorganotin hydrides with their non-toxic I germanium analogues for industrial generation of free-radicals in chain reactions. These germanium hydrides have similar reactivity to the corresponding tin hydrides and cantherefore act as substitutes in radical reactions. This will allow exploitation of the vast array of synthetic procedures, which require triorganotin hydrides as the free-radical generating reagent. New synthetic methods will be developed for the economic synthesis of the required triorganogermanium hydrides using the relatively cheap germanium oxide as the starting material.

The objectives of the project are:
- Development of the catalytic application of triorganogermanes for generation of free radicals.
- Synthesis of novel pharmaceuticals to test the methodology.

Training content (objective, benefit and expected impact)

Dr Bowman's research group is internationally known for free radical research and provides an excellent environment for furthering research training in radical chemistry and synthetic methodology related to pharmaceuticals to further the biological chemistry background of Dr Alcaraz.

Expected impact and benefit: We already have considerable industrial interest in the planned methodology and it will provide a facile and safe method for the pharmaceutical industry to use radical reactions in important syntheses.

Links with industry / industrial relevance (22)

The research group has long term industrial collaboration and discussions are underway with SmithKline Beecham with a view to developing the methodology, if fully successful, to the synthesis of an important drug under process development. The research should provide a facile, cheap and non-toxic new methodology for pharmaceutical synthesis using free radicals

Funding Scheme

RGI - Research grants (individual fellowships)

Coordinator

LOUGHBOROUGH UNIVERSITY
Address
Ashby Road
Loughborough
United Kingdom