¹⁸F-Labeling Using Click Cycloadditions

Figure 2

Radiosynthesis of a new amino-acid based ¹⁸F-prosthetic group (N-propargyl-2-amino-3-[¹⁸F]fluoro-propionic acid, “[¹⁸F]serine”) for ¹⁸F-CuAAC-labeling of complex biomolecules. (i) [K⊂2.2.2]⁺/¹⁸F⁻, DMSO, 140°C, 10 min; (ii) hydrochloric acid (3.3 M), 100°C, 15 min; for analytical purposes (sequential deprotection): (iii) sodium hydroxide (3.3 M), 60°C, 5 min; (iv) hydrochloric acid (3.3 M), 100°C, 15 min.