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Issue 2, 2013
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Flow chemistry synthesis of zolpidem, alpidem and other GABAA agonists and their biological evaluation through the use of in-line frontal affinity chromatography

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Abstract

The flow of information between chemical and biological research can present a bottleneck in pharmaceutical research. Tools that bridge these disciplines and aid information exchange have therefore clear value. Over the last few years, both synthetic chemistry and biological screening have benefited from automation, and a seamless chemistry–biology interface is now possible. We report here on the use of flow processes to perform synthesis and biological evaluation in an integrated manner. As proof of concept, a flow synthesis of a series of imidazo[1,2-a]pyridines, including zolpidem and alpidem, was developed and connected to a Frontal Affinity Chromatography screening assay to investigate their interaction with Human Serum Albumin (HSA).

Graphical abstract: Flow chemistry synthesis of zolpidem, alpidem and other GABAA agonists and their biological evaluation through the use of in-line frontal affinity chromatography

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Publication details

The article was received on 29 Oct 2012, accepted on 23 Nov 2012 and first published on 23 Nov 2012


Article type: Edge Article
DOI: 10.1039/C2SC21850J
Citation: Chem. Sci., 2013,4, 764-769
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    Flow chemistry synthesis of zolpidem, alpidem and other GABAA agonists and their biological evaluation through the use of in-line frontal affinity chromatography

    L. Guetzoyan, N. Nikbin, I. R. Baxendale and S. V. Ley, Chem. Sci., 2013, 4, 764
    DOI: 10.1039/C2SC21850J

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