High-throughput purification of single compounds and libraries

Journal of Combinatorial Chemistry
Mathias SchaffrathHans Ulrich Stilz

Abstract

The need for increasing productivity in medicinal chemistry and associated improvements in automated synthesis technologies for compound library production during the past few years have resulted in a major challenge for compound purification technology and its organization. To meet this challenge, we have recently set up three full-service chromatography units with the aid of in-house engineers, different HPLC suppliers, and several companies specializing in custom laboratory automation technologies. Our goal was to combine high-throughput purification with the high attention to detail which would be afforded by a dedicated purification service. The resulting final purification laboratory can purify up to 1000 compounds/week in amounts ranging from 5 to 300 mg, whereas the two service intermediate purification units take 100 samples per week from 0.3 to 100 g. The technologies consist of normal-phase and reversed-phase chromatography, robotic fraction pooling and reformatting, a bottling system, an automated external solvent supply and removal system, and a customized, high-capacity freeze-dryer. All work processes are linked by an electronic sample registration and tracking system.

References

Feb 22, 2001·Drug Discovery Today·M Jones
Jan 16, 2002·Drug Discovery Today·David Cork, Nick Hird
Mar 15, 2005·Journal of Combinatorial Chemistry·Angelika WeberHans Ulrich Stilz

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Citations

May 13, 2008·Drug Discovery Today·Alfonso EspadaMing-Shang Kuo
Sep 22, 2007·Current Opinion in Chemical Biology·Alan L Harvey
May 23, 2006·Drug Discovery Today·Marcus Koppitz, Knut Eis
May 2, 2014·Biotechnology Advances·Strahil BerkovPhilippe Christen
Jan 10, 2008·Journal of Combinatorial Chemistry·John Isbell
Jun 2, 2009·Journal of Biomolecular Screening·William P Janzen, Ioana G Popa-Burke
Sep 16, 2008·Journal of Combinatorial Chemistry·Oliver GuthKerstin Ilg
May 9, 2009·Journal of Combinatorial Chemistry·Julia FitzGibbonsLisa Schaffter
May 31, 2008·Journal of Combinatorial Chemistry·Marcus Koppitz

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