Easy access to heterobimetallic complexes for medical imaging applications via microwave-enhanced cycloaddition

• Nicolas Desbois,
• Sandrine Pacquelet,
• Adrien Dubois,
• Clément Michelin and
• Claude P. Gros

Beilstein J. Org. Chem. 2015, 11, 2202–2208, doi:10.3762/bjoc.11.239

• ” reaction, has been applied to the synthesis of a range of triazole-linked porphyrin/corrole to DOTA/NOTA derivatives. Microwave irradiation significantly accelerates the reaction. The synthesis of heterobimetallic complexes was easily achieved in up to 60% isolated yield. Heterobimetallic complexes were

• are promising contrast agents (CA) in MRI. Keywords: click chemistry; corrole; DOTA; microwave; NOTA; porphyrin; Introduction Magnetic resonance imaging (MRI), positron emission tomography (PET) or single photon emission computed tomography (SPECT) are actually the most commonly used imaging

• alkynes e.g. a propargyl-DOTA-tris(t-Bu)ester and a propargyl-NOTA(t-Bu)2. Indeed, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA, 3) and 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA, 4) are well-known to form highly stable Gd(III) and Ga(III) complexes and they are intensely studied