Hetero Multifunctional linkers

Heteromultifunctional cross-linking reagents are molecules of great importance for bioconjugation, diagnosis, therapy and layer functionalization. Despite their attractiveness, a few structures displaying more than 2 different functionalities are described. The project aims at synthesizing new heteromultifunctional linkers displaying up to four functional groups able to undergo bioorthogonal modifications, in respect to the concept of click chemistry.  The strategy to access this valuable compounds includes environmental and industrial considerations and is based on a novel double functionalization of nitriles using zinc chemistry.

By aiming application in diagnostic imaging, therapy and even theranostic, this project is developed in collaboration with Raphaël Tripier (CEMCA, Université de Bretagne Occidentale) and the start-up EasyChelators for the grafting of saturated azamacrocycles able to chelate cations (64Cu and 67Cu for positron emission tomography or targeted nuclear medicine for instance).

Researchers

• Fabien Boeda
• Morwenna Pearson-Long
• Philippe Bertus

Related papers

• Polyfunctional compounds, methods for their preparing same and uses thereof

Composés multifonctionnels, leurs procédés de préparation et leurs utilisations, Bertus, L. Fontaine, M. S. M. Pearson-Long, F. Boeda, J. Caillé, V. Gaignet

• Demande de brevet n° FR2016-57227, déposée le 27 juillet 2016

WO 2017-EP66675, 4 juillet 2017

Publication : Patent WO 2018/019527A, publiée le 01 février 2018