Total solid-phase synthesis of 1,4,7,10-tetraazacyclododecane-N,N', N',N'-tetraacetic acid-functionalized peptides for radioimmunotherapy |
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Authors: | Peterson J J Pak R H Meares C F |
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Institution: | Department of Chemistry, University of California, One Shields Avenue, Davis, California 95616-5295, USA. |
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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. |
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