omation mbers - Society for Laboratory Automation and Screening

10:30 am Wednesday, February 4 HT Chemistry – Microscale Room B3
Miryam Fernandez Suarez
GlaxoSmithKline Pharmaceuticals
GSK, CTC, University Chemical Labs
Lensfield Road
Cambridge, CB2 1EW United Kingdom
miryam_2_fernandez-suarez@gsk.com
Microfluidic Platforms for Drug Discovery
49
Co-Author(s)
Stephanie Y. F. Wong
Brian H. Warrington
The competitive world of drug market, under cost reduction pressures and imminent expiration of patents, forces
pharmaceutical companies to an expensive search for suitable novel leads. Combinatorial chemistry and high
throughput screening have proved to be useful for discovering potential drug candidates. However, these costly
techniques did not satisfy the high expectations in terms of number of drug candidates entering development
stages, as they hardly scratch the enormous and diverse universe of the possible compounds and even can lead
to logistic problems of reagent consumption, sample storage and waste production. In response to the competing
pressures for increasing output and reducing time scales and costs, the pharmaceutical industry is in the midst of
a technology-driven revolution. In this contest, microfluidic based technologies show a great potential owing to its
high degree of integration with modern miniaturised analysis and screening techniques. It also offers advantages
in terms of shorter response times, reduction of reagent consumption and waste volume. Our aim is to perform
multiple functions such as synthesis, detection, separation, and screening all integrated in a microfabricated
device, exploiting the advantages of combining microfluidics and electronic components and provided with
software tools for optimization. In this presentation, we will review the approach of GSK and partners to exploit
the advantages of microfluidics in the development of miniaturized chemistry platforms, from our initial well-based
approaches, to our continuous flow automated micro reactor systems. In addition, we will present our latest
developments towards multi-step synthesis protocols and coupling with screening assays.
11:00 am Wednesday, February 4 HT Chemistry – Microscale Room B3
Mike Pollard
Syrris
27 Jarman Way
Royston, Herts, SG8 5HW United Kingdom
mike.pollard@syrris.com
Real-world Microchemistry: Milligram Scale Organic Synthesis in Microreactors
Microreactors are an emerging technology, offering great promise for productivity gains in drug discovery and
development. Some early presentations made promises of “magic” gains in yield and reaction speed, claimed as
achievable as a direct result of the channel geometry and fluidic design of these devices. However, these gains
have not been consistently demonstrated. Medicinal chemists have rightly remained sceptical that a chip-based
reactor system can offer ease of use coupled with delivering a realistic quantity of the desired compound. Syrris
has now been working for two years to develop the technologies needed to make Microreactors a real world
proposition. From the start of its development program, Syrris has focused on the medicinal chemist’s need for
a robust, practical, low cost tool, capable of reliably synthesising milligram quantities of compound. We have
recently carried out an extensive test program to validate the performance of Syrris Microreactor chips over a wide
range of organic synthesis tasks. The tests addressed issues such as: the range of synthesis protocols that could
be undertaken, reaction rate, yield, and automatically handling real world problems such as precipitation. This
paper presents details of the synthesis work carried out, including a realistic assessment of the best application
area for Microreactors. We will present a preview of the forthcoming Syrris AutoR medicinal chemistry tool,
being developed as part of our strategy to understand and meet the needs of the R&D scientist though research,
collaboration, and product development.
PODIUM ABSTRACTS