Scale-Up of Flow-Assisted Synthesis of C2-Symmetric Chiral PyBox Ligands

    Claudio Battilocchio1,3, Marcus Baumann1, Ian R. Baxendale1, Mariangela Biava3, Matthew O. Kitching1, Steven V. Ley1, Rainer E. Martin*2, Stephan A. Ohnmacht2, Nicholas D. C. Tappin1

    • 1Department of Chemistry, University of Cambridge, UK
    • 2F. Hoffmann-La Roche Ltd., Pharmaceuticals Division, Basel, Switzerland
    • 3Department of Pharmaceutical Chemistry and Technology, Sapienza University of Rome, Italy

    A series of PyBox ligands were prepared from commercially available chelidonic acid by a multistep flow sequence using mesoreactor technology. A chloro group introduced onto the ligand scaffold was subsequently exploited to give amine derivatives ready for immobilization through microencapsulation technologies.

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