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Details of Grant 

EPSRC Reference: GR/M87627/01
Title: CATALYTIC ALKENE METATHESIS IN PHARMACEUTICAL SYNTHESIS
Principal Investigator: Barrett, Professor T
Other Investigators:
Chadwick, Professor D
Researcher Co-Investigators:
Project Partners:
GlaxoSmithKline plc (GSK)
Department: Chemistry
Organisation: Imperial College London
Scheme: LINK
Starts: 01 November 1999 Ends: 31 October 2001 Value (£): 140,601
EPSRC Research Topic Classifications:
Catalysis & Applied Catalysis
EPSRC Industrial Sector Classifications:
Pharmaceuticals and Biotechnology
Related Grants:
Panel History:  
Summary on Grant Application Form
Alkene metathesis reactions will be applied for the synthesis and subsequent manufacture of serine protease inhibitors for application as drugs for the treatment of chronic obstructive pulmonary disease and viral infections. In the key step, ring closing or crossed metathesis using C12 (Cy3P) 2Ru=CHPh and related supported catalysts will be used to prepare key pharmaceuticals using inexpensive starting materials and providing intermediates with minimal waste stream. The methods will be applicable to small scale use in a combinatorial approach for the discovery of new generation analogues following biological evaluation. Currently, synthetic procedures used by medicinal chemists in drug discovery are massively different to the synthetic procedures used on scale-up which in turn are very different from the exact chemistry used in the manufacturing process. There are considerable time and economic advantages in minimising this charge and the development of seamless synthetic methodology for discovery to manufacture is indeed a glittering prize.
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Further Information:  
Organisation Website: http://www.imperial.ac.uk