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Details of Grant 

EPSRC Reference: GR/S90904/01
Title: Solid phase synthesis: an advantageous approach to isotopically labelled substances
Principal Investigator: Spivey, Professor A
Other Investigators:
Researcher Co-Investigators:
Project Partners:
Department: Chemistry
Organisation: Imperial College London
Scheme: Standard Research (Pre-FEC)
Starts: 01 October 2004 Ends: 30 September 2007 Value (£): 108,558
EPSRC Research Topic Classifications:
Chemical Synthetic Methodology
EPSRC Industrial Sector Classifications:
Chemicals Pharmaceuticals and Biotechnology
Related Grants:
Panel History:  
Summary on Grant Application Form
The preparation of isotopically labelled analogues of potential medicines forms an integral part of the complex process of medicine discovery. Isotopically labelled compounds are used in studies to determine the possible toxic side effects associated with medicines. Their preparation is a hazardous and expensive buisness because labelled intermediates are toxic and require rigorous containment. Issues of containment are most acute during the first steps in a synthesis because these involve handling volatile labelled starting materials and intermediates. It is proposed here to develop protocols for the devolatilisation of these chemicals by direct immobilisation of the labelled precursor onto a polymeric support. The advantage for the radiochemist is that contamination by inhalation is no longer possible. The advantage for the public and the environment is that labelled fume-hood exhaust emissions are eliminated. The advantage commercially is that expensive isotopic label is not lost and the risk of costly litigation arising from health and environmental accidents is reduced.Additionally, certain isotopically labelled fluorine-containing compounds are used extensively in brain research and as imaging agents in a type of medical imaging process known as PET scanning. PET scans are available in major UK hospitals for diagnosis of e.g. Parkinson's disease and schizophrenia. The imaging compounds used have to be made 'on-site' in hospitals, and it is proposed here to develop a method for the direct preparation of this type of isotopically labelled compound. In particular, the method will be rapid, efficient and provide the pure products directly for use. This will circumvent the use of the toxic precursors as presently employed and moreover will avoid the need for costly and time-consuming purification that currently limit the 'activity' of the labelled compounds and hence the quality of the final scans.
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Organisation Website: http://www.imperial.ac.uk