Chemoselective ¹⁸F-incorporation into pyridyl acyltrifluoroborates for rapid radiolabelling of peptides and proteins at room temperature
2020
Chiotellis, Aristeidis | Ahmed, Hazem | Betzel, Thomas | Tanriver, Matthias | White, Christopher J. | Song, Haewon | Da Ros, Sara | Schibli, Roger | Bode, J. W. (Jeffrey W.) | Ametamey, Simon M.
A new prosthetic group is reported for ¹⁸F-labelling of peptides and proteins based on the chemoselective ligation of potassium acyltrifluoroborates (KATs) and hydroxylamines without any detectable ¹⁸F/¹⁹F isotope exchange at the acyltrifluoroborate moiety. The new building block is appended via a common amide bond at room temperature with no need for protecting groups which enables an effective orthogonal ¹⁸F-radiolabelling.
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