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A machine-assisted approach for the preparation of follow-on pharmaceutical compound libraries

Schotten, Christiane, Leist, Lisa G. T., Semrau, Anna Lisa and Browne, Duncan L. 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
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: 18 Jan 2021 22:53
URI: http://orca.cardiff.ac.uk/id/eprint/109364

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