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- Title
Efficient Synthesis of 1,4,7-Triazacyclononane and 1,4,7-Triazacyclononane-Based Bifunctional Chelators for Bioconjugation.
- Authors
Désogère, Pauline; Rousselin, Yoann; Poty, Sophie; Bernhard, Claire; Goze, Christine; Boschetti, Frédéric; Denat, Franck
- Abstract
The reaction of diethylenetriamine with chloroacetaldehyde yielded a bicyclic aminal intermediate for the synthesis of 1,4,7-triazacyclononane (TACN), a macrocyclic polyamine the derivatives of which find applications as catalysts, bleaching agents, and chelators for medical imaging. This new synthetic protocol outperforms the synthetic methods described so far because it does not involve any cyclization step. Moreover, this aminal intermediate allowed access to a new family of TACN derivatives functionalized on the carbon skeleton, for example, C-aminomethyl-TACN. This novel compound is a precursor of valuable bifunctional chelating agents for nuclear medicine, in particular, for the preparation of PET imaging agents after bioconjugation and metallation with 68Ga or 64Cu.
- Subjects
CHEMICAL synthesis; TRIAZACYCLONONANE; POLYAMINES; IRON chelates; BIOCONJUGATES
- Publication
European Journal of Organic Chemistry, 2014, Vol 2014, Issue 35, p7831
- ISSN
1434-193X
- Publication type
Article
- DOI
10.1002/ejoc.201402708