Patent ID: 8795631

Claim:
A radiofluorination method comprising: (i) radiofluorination of an azide of Formula Ia with a suitable source of [ 18 F]-fluoride ion to obtain a radiofluorinated azide of Formula Ib: wherein said radiofluorination is carried out in a solvent suitable for said radiofluorination, and wherein; R 1 is C 1-10 alkylene, C 3-10 cycloalkylene, C 4-20 cycloalkylene-alkylene, C 5-14 arylene, C 6-20 alkylene-arylene, C 1-10 heteroalkylene, C 2-10 heterocycloalkylene, C 3-13 heteroarylene, C 6-20 heteroalkylene-arylene, C 6-20 alkylene-heteroarylene, or C 6-20 heteroalkylene-heteroarylene, wherein R 1 has between 0-3 substituents selected from C 1-4 alkyl, C 5-10 aryl, amino, hydroxy, halo or nitro; and, wherein R 1 optionally comprises one or more protecting groups; and LG is a suitable leaving group; (ii) reduction of the radiofluorinated azide of Formula Ib to obtain a radiofluorinated amine of Formula Ic: H 2 N—R 1 — 18 F (Ic) wherein said reduction is carried out in a solvent suitable for said reduction and catalysed by elemental copper in the presence of an acid; and wherein R 1 is as defined in step (i).