Total Solid-Phase Synthesis of 1,4,7,10-Tetraazacyclododecane-N,N‘,N‘‘,N‘‘‘-tetraacetic Acid-Functionalized Peptides for Radioimmunotherapy

Publisher Website
Google Scholar
Abstract
A convenient approach to the functionalization of peptides with the macrocyclic 1,4,7,10-tetraazacyclododecane-N,N‘,N‘ ‘,N‘ ‘‘-tetraacetic acid (DOTA) moiety has been developed. Protected components (using tert-butyl or tert-butyloxycarbonyl groups) of both the peptide and the chelate were assembled on the same solid resin support. Deprotection and cleavage of the resin-bound DOTA−peptides were performed in one step using a trifluoroacetic acid cleavage mixture to yield free DOTA−peptide amides.