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

Claudio Battilocchio^1,3, 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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