Details of Grant 

EPSRC Reference:	EP/I038489/1
Title:	Development of a General sp2-sp3 Coupling Methodology
Principal Investigator:	Stockman, Professor RA
Other Investigators:
Researcher Co-Investigators:
Project Partners:
Department:	Sch of Chemistry
Organisation:	University of Nottingham
Scheme:	Standard Research
Starts:	01 October 2011	Ends:	30 September 2015	Value (£):	141,893
EPSRC Research Topic Classifications:	Chemical Synthetic Methodology
EPSRC Industrial Sector Classifications:
Related Grants:
Panel History:	Panel Date Panel Name Outcome 12 May 2011 EPSRC Physical Sciences Chemistry* Announced
Summary on Grant Application Form
2010 saw the award of the Nobel Prize for Chemistry to Negishi, Suzuki and Heck for the palladium-catalysed cross coupling between aryl halides and other aryl / alkene systems. Over the past 20 years, sp2-sp2 couplings have changed the way in which the Pharmaceutical industry builds molecules, and thus are rightly deserving of this highest award. Furthermore, these couplings have proven to be tolerant of a wide range of functional groups, solvents, and substrates, making them a general solution to the synthesis of biaryls and aryl-alkenes. Currently, the desire for inclusion of more sp3 atoms within lead compounds has never been higher, with a number of studies confirming that compounds which have more three-dimensionality have a lower attrition rate on the long journey to become a new chemical entity. With current attrition rates around the 97% level, any small lowering of this could have a huge economic impact on the Pharmaceutical sector. Thus attention has turned to adaptation of the existing palladium-catalysed coupling technologies to the formation of sp2-sp3 coupled products. Whilst there are some notable methodologies within this relatively young field of research, there has yet to emerge a general and reliable method to couple aryl and alkyl groups. This programme of research will take a number of preliminary findings and transform these into a general and flexible methodology for the synthesis of aryl and heteroaryl rings coupled to stereogenic sp3 alkyl groups. Unlike the majority of research in this area, this new methodology will not rely on palladium or other expensive / toxic metals as catalysts, but rather delineate a method which exploits the underdeveloped chemistry of sulfoxides. This will therefore be complementary to other methodologies being investigated around the world.
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Organisation Website:	http://www.nottingham.ac.uk