S-Trityl protection of bis-amino bis-thiol (BAT) chelator enables flexible derivatisation and facile labelling with technetium-99m

We have coupled S, S′-bis-trityl N-BOC protected 1,2-ethylenedicysteamine, a bis-amino bis-thiol (BAT) tetraligand, via a propylene or ethylene spacer to several biologically active molecules including 2-nitroimidazole, desethylflumazenil, a beta-CIT analogue, glucose and 2-(2′-hydroxy-4′-aminopheny...

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Bibliographic Details
Published in:Tetrahedron letters 2003-03, Vol.44 (12), p.2597-2600
Main Authors: Cleynhens, Bernard J., Bormans, Guy M., Vanbilloen, Hubert P., Vanderghinste, Dominique V., Kieffer, Davy M., de Groot, Tjibbe J., Verbruggen, Alfons M.
Format: Article
Language:English
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Summary:We have coupled S, S′-bis-trityl N-BOC protected 1,2-ethylenedicysteamine, a bis-amino bis-thiol (BAT) tetraligand, via a propylene or ethylene spacer to several biologically active molecules including 2-nitroimidazole, desethylflumazenil, a beta-CIT analogue, glucose and 2-(2′-hydroxy-4′-aminophenyl)-1,3-benzothiazole. The conjugates were efficiently labelled with technetium-99m by consecutive heating of the S, S′-bis-trityl protected ligand in hydrochloric acid followed by neutralisation and heating in the presence of 99mTc-tartrate. The S, S′-bis-trityl BAT chelator is an interesting synthon that allows both flexible derivatisation with various biologically active molecules and facile labelling with technetium-99m. Labelling of, S, S′-bis-trityl- N-BOC BAT with technetium-99m.
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(03)00224-7