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Fine Chemicals Group




GPCRs in Medicinal Chemistry

8 - 10 September 2008

GPCRs in Medicinal Chemistry




High throughput theme is all part of the process

Fine Chemicals Group: Process development symposium, 2006

Back row (L to R) Linda Woodcock, Lee Challinor, Phillip Parker, Sean Parris, Matthew McConville. Middle (L to R) Greg Stepney, Nicola Gardner, Nathan Owston, Stephen Rowbottom, Franziska Schoenbeck. Front (L to R) Stephen Moore, Gemma Turner, Jennifer Slaughter. Carles Giro-Manas also attended.
Back row (L to R) Linda Woodcock, Lee Challinor, Phillip Parker, Sean Parris, Matthew McConville. Middle (L to R) Greg Stepney, Nicola Gardner, Nathan Owston, Stephen Rowbottom, Franziska Schoenbeck. Front (L to R) Stephen Moore, Gemma Turner, Jennifer Slaughter. Carles Giro-Manas also attended.

The process development symposium meeting, organised by SCI’s Fine Chemicals Group and held at Churchill College, Cambridge, UK in December 2006 attracted more than 180 international delegates and welcomed 14 PhD students who were able to attend assisted by industry bursaries.

Presentations covered a wide range of scientific subjects, with talks varying from ‘academic’ to highly ‘applied’ topics. A mix of case histories by speakers from the pharmaceutical industry demonstrated how modern synthetic methodologies and the increasing use of enabling technologies are being used to design processes that continue to address quality, economics and safety challenges in addition to increased focus on reducing waste.

An emerging theme at the meeting was the growing use of combinatorial techniques for the high throughput synthesis and screening of ligands, catalysts and conditions for applications in asymmetric reactions. David Ager from DSM Pharma Chemicals discussed the use of high throughput experimentation coupled with fundamental mechanistic understanding in the identification of novel phosphoamidite ligands and their use in asymmetric hydrogenation and boronic acid additions.

Following a similar theme of high throughput experimentation, Barry Lygo from Nottingham University presented his work on the identification of novel chiral phase transfer catalysts and their use in the synthesis of homo chiral amino acids and natural products. For this work Lygo, an SCI member, received the 2006 UK Prize for Process Chemistry Research, sponsored by AstraZeneca, Pf izer and GlaxoSmithKline.

Karl Anker Jorgensen from Aarhus University, Denmark provided an insight into the topical area of organocatalysis including its use in multicomponent reactions. In contrast, Cranf ield University’s Sergey Piletsky discussed the less well known and emerging area of molecular imprints as catalysts and solid phase extractants.

The meeting set out a number of challenges, particularly to the pharmaceutical industry. Frank Montgomery looked at how AstraZeneca is addressing the recent concept of design space filings to demonstrate quality control in the manufacture of new active pharmaceutical ingredients, while Gawayne Mahboubian- Jones from Optimal Industrial Automation challenged the pharmaceutical industry over why it does not use in-line process analytical techniques to generate real time reaction data and demonstrate control throughout the whole process. Finally, Mark Dickson of Foster Wheeler Energy discussed continuous chemistry, encouraging its wider application in the pharmaceutical industry.

Alan Pettman,
Pfizer Global Research and Development