Synthesis of a Drug-Like Focused Library of Trisubstituted Pyrrolidines Using Integrated Flow Chemistry and Batch Methods

    • Marcus Baumann1
    • Ian R. Baxendale1
    • Steven V. Ley1
    • Christoph Kuratli2
    • Rainer E. Martin2
    • Josef Schneider2
    • 1Innovative Technology Centre, University of Cambridge, U.K.
    • 2F. Hoffmann-La Roche Ltd., Basel, Switzerland

    A combination of flow and batch chemistries has been successfully applied to the assembly of a series of trisubstituted drug-like pyrrolidines. This study demonstrates the efficient preparation of a focused library of these pharmaceutically important structures using microreactor technologies, as well as classical parallel synthesis techniques, and thus exemplifies the impact of integrating innovative enabling tools within the drug discovery process.

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