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. 2010 Mar 14;46(10):1706-8.
doi: 10.1039/b924784j. Epub 2010 Feb 6.

Clickable bifunctional radiometal chelates for peptide labeling

Artem Y Lebedev  1 , Jason P Holland, Jason S Lewis
Affiliations

Clickable bifunctional radiometal chelates for peptide labeling

Artem Y Lebedev et al. Chem Commun (Camb). .

Abstract

Novel synthetic methods for producing an array of chelates for use in "click"-radiolabeling of peptides are described, and their reactivity with regards to subsequent conjugation and radiolabeling is discussed.

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Figures

Fig. 1
Fig. 1
DFT optimized structure of the hypothetical model complex. r(Cu⋯N3) = 2.559 Å; r(Cu–N4) = 2.110 Å; r(Cu–N5) = 2.092 Å; r(Cu–N7) = 2.299 Å; r(Cu–O1) = 1.930 Å.
Scheme 1
Scheme 1
Synthesis of the “clickable” chelates. (i) See ESI for full details.
Scheme 2
Scheme 2
“Click” conjugation onto the model peptide. (i) CuCl2, ascorbic acid in water, RT; (ii) trifluoroacetic acid, iPr3SiH, EDT.
See this image and copyright information in PMC

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