Schotten, C, Leist, LGT, Semrau, AL et al. (1 more author) (2018) A machine-assisted approach for the preparation of follow-on pharmaceutical compound libraries. Reaction Chemistry & Engineering, 3 (2). pp. 210-215.
Abstract
Follow-on drugs represent the majority of new drug introductions and show improved properties to the pioneer drug. In order to fast-follow, R&D needs to be able to quickly generate a library of analogues that can then be screened for desired properties. Here we have designed a hybrid machine-assisted approach which makes use of both multi-step continuous flow processing and robotic microwave reactors to generate a library of indoles over two technology steps (four reaction steps; diazotization, reduction, unmasking of the hydrazine and Fischer indole reaction). This ‘machine’ is then used to prepare a small library of hitherto unreported analogues of the 5-HT agonist Zolmitriptan in good yields, thus demonstrating that the integration and use of machines is a powerful tool to expedite drug discovery.
Metadata
Item Type: | Article |
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Authors/Creators: |
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Dates: |
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Institution: | The University of Leeds |
Academic Units: | The University of Leeds > Faculty of Engineering & Physical Sciences (Leeds) > School of Chemistry (Leeds) > Inorganic Chemistry (Leeds) |
Depositing User: | Symplectic Publications |
Date Deposited: | 12 Jun 2018 15:34 |
Last Modified: | 12 Jun 2018 15:34 |
Status: | Published |
Publisher: | Royal Society of Chemistry |
Identification Number: | 10.1039/C8RE00010G |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:131875 |