Schotten, Christiane, Leist, Lisa G. T., Semrau, Anna Lisa and Browne, Duncan L. ORCID: https://orcid.org/0000-0002-8604-229X 2018. A machine-assisted approach for the preparation of follow-on pharmaceutical compound libraries. Reaction Chemistry and Engineering 3 (2) , pp. 210-215. 10.1039/C8RE00010G |
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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.
Item Type: | Article |
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Date Type: | Published Online |
Status: | Published |
Schools: | Chemistry |
Publisher: | Royal Society of Chemistry |
ISSN: | 2058-9883 |
Date of First Compliant Deposit: | 21 February 2018 |
Date of Acceptance: | 9 February 2018 |
Last Modified: | 07 Nov 2023 04:50 |
URI: | https://orca.cardiff.ac.uk/id/eprint/109364 |
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