Parallel purification of microscale libraries via automated solid phase extraction

High-throughput experimentation (HTE) has become more widely utilized in drug discovery for rapid reaction optimization and generation of large synthetic compound arrays. While this has accelerated medicinal chemistry design, make, test (DMT) iterations, the bottleneck of purification persists, cons...

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Bibliographic Details
Published in:SLAS technology 2024-04, Vol.29 (2), p.100126-100126, Article 100126
Main Authors: Wleklinski, Michael, Carpenter, Paige M., Dykstra, Kevin D., Donofrio, Anthony, Nowak, Timothy, Krska, Shane W., Ferguson, Ronald D.
Format: Article
Language:English
Subjects:
Amides
Analytical
Automation
Drug Discovery
HTE
Parallel purification
Parallel synthesis
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Summary:High-throughput experimentation (HTE) has become more widely utilized in drug discovery for rapid reaction optimization and generation of large synthetic compound arrays. While this has accelerated medicinal chemistry design, make, test (DMT) iterations, the bottleneck of purification persists, consuming time and resources. Herein we describe a general parallel purification approach based on solid phase extraction (SPE) that provides a more efficient and sustainable workflow producing compound libraries with significantly upgraded purity. This robust, user-friendly workflow is fully automated and integrated with HTE library synthesis, as demonstrated by its application to a diverse parallel library compound array generated via amide-bond coupling in HTE microscale format.
ISSN:2472-6303
2472-6311
DOI:10.1016/j.slast.2024.100126