Issue 23, 2008

Synthesis of Gd(III)-C-palmitamidomethyl-C′-DOTAMA-C6-o-carborane: a new dual agent for innovative MRI/BNCT applications

Abstract

C-(2-Benzyloxy)-ethyl-C′-N-tert-butoxycarbonyl-aminomethyl-o-carborane (8), a potentially useful intermediate for BNCT, has been synthesised. This intermediate can be readily functionalised with several biological vectors and MRI contrast agents. In this work intermediate 8 has been functionalised with a palmityl chain for lipophilic targeting and with Gd(III)-DOTAMA-C6-NH2 as MRI detector. This combination yielded Gd(III)-C-palmitamidomethyl-C′-DOTAMA-C6-o-carborane (14) as a dual MRI-BNCT agent.

Graphical abstract: Synthesis of Gd(III)-C-palmitamidomethyl-C′-DOTAMA-C6-o-carborane: a new dual agent for innovative MRI/BNCT applications

Supplementary files

Article information

Article type
Paper
Submitted
27 May 2008
Accepted
22 Sep 2008
First published
24 Oct 2008

Org. Biomol. Chem., 2008,6, 4460-4466

Synthesis of Gd(III)-C-palmitamidomethyl-C′-DOTAMA-C6-o-carborane: a new dual agent for innovative MRI/BNCT applications

S. Aime, A. Barge, A. Crivello, A. Deagostino, R. Gobetto, C. Nervi, C. Prandi, A. Toppino and P. Venturello, Org. Biomol. Chem., 2008, 6, 4460 DOI: 10.1039/B808804G

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