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New publication of COSM team : Synthesis of Orthogonal N-Protected C-functional Side-Bridged Cyclams to give access to unsymmetrical constrained BCAs

Thomas Le Bihan, Nathalie Le Bris,* Hélène Bernard, Carlos Platas-Iglesias, Raphaël Tripier*

DOI: 10.1002/ejoc.201901013

Considering the current importance of unsymmetrical mono- and di-N-functionalized ethylene side-bridged (sb) cyclams and the need to have their C-appended derivatives bearing an additional function dedicated to a conjugation to an external moiety as a targeting biomolecule, we have developed a general procedure to obtain orthogonally N-protected sb‑cyclams with a benzyl or a Boc group. Despite the lack of symmetry of the compounds, this methodology allows the specific protection of one or the other remaining secondary amine function.