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Issue 2, 2018
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A machine-assisted approach for the preparation of follow-on pharmaceutical compound libraries

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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.

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

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Publication details

The article was received on 26 Jan 2018, accepted on 09 Feb 2018 and first published on 16 Feb 2018


Article type: Paper
DOI: 10.1039/C8RE00010G
Citation: React. Chem. Eng., 2018,3, 210-215
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    A machine-assisted approach for the preparation of follow-on pharmaceutical compound libraries

    C. Schotten, L. G. T. Leist, A. L. Semrau and D. L. Browne, React. Chem. Eng., 2018, 3, 210
    DOI: 10.1039/C8RE00010G

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