10.1021/bc0600564.s001
Jan Marik
Jan
Marik
Sven H. Hausner
Sven H.
Hausner
Lauren A. Fix
Lauren A.
Fix
M. Karen J. Gagnon
M.
Karen J. Gagnon
Julie L. Sutcliffe
Julie L.
Sutcliffe
Solid-Phase Synthesis of 2-[<sup>18</sup>F]Fluoropropionyl Peptides
American Chemical Society
2006
prosthetic group
HPLC purification
positron emission tomography
peptide
phase support
radiolabeling proteins
175 min
2006-07-19 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Solid_Phase_Synthesis_of_2_sup_18_sup_F_Fluoropropionyl_Peptides/3070063
The 2-[<sup>18</sup>F]fluoropropionic (2-[<sup>18</sup>F]FPA) acid is used as a prosthetic group for radiolabeling proteins and peptides
for targeted imaging using positron emission tomography (PET). Radiolabeling of compounds with more than
one acylable functional group can lead to complex mixtures of products; however, peptides can be labeled
regioselectively on the solid phase. We investigated the use of a solid-phase approach for the preparation of
2-[<sup>18</sup>F]fluoropropionyl peptides. [<sup>18</sup>F]FPA was prepared and conjugated to the peptides attached to the solid phase
support. The <sup>18</sup>F-labeled peptides were obtained in 175 min with decay corrected yields of 10% (related to [<sup>18</sup>F]fluoride) and with a purity of 76−99% prior HPLC purification. The suitability of various coupling reagents and
solid supports were tested for radiolabeling of several peptides of various lengths.