Issue 37, 2016

Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK

Abstract

Solid-phase peptide synthesis, head-to-tail cyclization, and subsequent radiolabeling provided a reproducible, simple, rapid synthetic method to generate the cyclic peptide radiotracer cRGDyK([18F]FBA). Herein is reported the first on-resin cyclization and 18F-radiolabeling of a cyclic peptide (cRGDyK) in an overall peptide synthesis yield of 88% (cRGDyK(NH2)) and subsequent radiolabeling yield of 14 ± 2% (decay corrected, n = 4). This approach is generally applicable to the development of an automated process for the synthesis of cyclic radiolabeled peptides for positron emission tomography (PET).

Graphical abstract: Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK

Supplementary files

Article information

Article type
Communication
Submitted
29 Jul 2016
Accepted
25 Aug 2016
First published
25 Aug 2016

Org. Biomol. Chem., 2016,14, 8659-8663

Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK

R. A. Davis, K. Lau, S. H. Hausner and J. L. Sutcliffe, Org. Biomol. Chem., 2016, 14, 8659 DOI: 10.1039/C6OB01636G

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