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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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Article information


Submitted
29 Oct 2012
Accepted
23 Nov 2012
First published
23 Nov 2012

Chem. Sci., 2013,4, 764-769
Article type
Edge Article

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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