18 F-prosthetic groupSteps/reaction time RCY Reacting agent Reaction type/ catalytic system Overall reaction time1 (CCA) RCY CCA Literature C -(4-
18 F
fluoro-phenyl)-N-phenyl-nitrone
2 steps/20 min, (labeling of
18 F
FB-CHO: 1 step, 50 min)
22–37%1 (
18 F
FB-CHO: 30–50%) (18 F-nitrone: 74%) Various maleimides 80 min (10 min) 87–91% [19 ]
4-
18 F
fluoro-benzonitrile oxide
3 steps/20 min (labeling of
18 F
FB-CHO: 1 step, 50 min)
28–46%1 (
18 F
FB-CHO: 30–50%) (18 F-nitro oxide: 92%) Various dipolarophiles
1,3-dipolar
3+2
cycloaddition, no catalyst
80 min (10 min) 36–99%
[20 ] Cyclononyne-indomethacins (COX-2 inhibitor) 81% Maleimide-indomethacins (COX-2 inhibitor) 55% Propyne-indomethacins (COX-2 inhibitor) 35% N -hydroxy-4-
18 F
fluorobenz-imidoyl chloride4 steps/20 min (labeling of
18 F
FB-CHO: 1 step, 50 min) 27–45%1 (
18 F
FB-CHO: 30–50%) (18 F-nitro oxide: 92%) (18 F-benzimidoyl Cl: 99%) Cyclononyne-
-Ala-Phe-OMe (dipeptide) 85 min (10 min) 88%2 Norbornene-
-Ala-Phe-OMe (dipeptide) 82%2 C -(4-
18 F
fluoro-phenyl)-N-phenyl-nitrone
2 steps/20 min, (labeling of
18 F
FB-CHO: 1 step, 50 min)
22–37%1 (
18 F
FB-CHO: 30–50%) (18 F-nitrone: 74%) Terminal alkynes methyl propiolate radio -Kinugasa, CuSO4 , AscONa (L -histidine)80 min (10 min) 89% (trans/cis = 2 : 3)
[21 ] Terminal alkyne propargyl alcohol radio -Kinugasa, CuI (CuI -stabilizing ligands or pyridine)
100 min (30 min) 82% (trans/cis = 1 : 5) 60% (trans/cis = 1 : 5) Terminal alkyne 1-propargyl uracyl (nucleobase chimera) 65% (trans/cis = 4 : 1) propiolyl-
-Ala-Phe-OMe (dipeptide) radio -Kinugasa, CuSO4 , AscONa (L -histidine)
80 min (10 min) 85% (trans/cis = 1 : 3) propiolated protein (BSA) 32% o -/p -
18 F
fluoro-phenyl acetylenen.d. n.d. 3,6-dihydro-2H -1,4-oxazine-4-oxide radio -Kinugasa, CuI (1,10-phenanthroline)(10 min) 52% (ortho ) 41% (para )