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. Author manuscript; available in PMC: 2023 Apr 7.
Published in final edited form as: J Labelled Comp Radiopharm. 2018 Feb 5;61(3):196–227. doi: 10.1002/jlcr.3570

TABLE 2.

Some labeling synthons prepared from aryliodonium ylides

graphic file with name nihms-1887903-t0025.jpg
Entry Labeling Synthon Precursor
Labeling Conditions
Yield,b % References
R1 Auxa Mode Solvent °C min
1 [18F]3-Fluorobromobenzene 3-Br C Batch DMF 130 10 72 ± 3 Yuan et al115
2 [18F]4-Fluoroiodobenzene 4-I A Batch DMSO 110 15 70 ± 10 Kügler et al101
3 [18F]3-Fluorobenzaldehyde 3-CHO B Batch DMF 120 10 7-52 Petersen et al116
4 [18F]3-Fluorobenzyl azide 3-CH2N3 B Batch DMF 120 ns 69 ± 8 Wang et al117
5 [18F]4-Fluorobenzyl azide 4-CH2N3 B Batch DMF 120 10 70 ± 4 (52 ± 2)
6 [18F]4-Fluorobenzyl azide 4-CH2N3 B Batch DMF 120 10 (25 ± 10) c Rotstein et al67
7 [18F]4-Fluorobenzyl azide 4-CH2N3 B MR DMF 210 ~1 68 ± 5 (24 ± 0) Calderwood et al75
8 [18F]3-Fluorobenzoic acid methyl ester 3-CO2Me B Batch DMF 120 10 77 ± 7 Rotstein et al67
9 [18F]2-(3-Fluorophenyl)ethylamined 3-(CH2)2NHBoc A Batch DMF 110 10 ~70 Drerup et al118
graphic file with name nihms-1887903-t0026.jpg
10 [18F]1-(2-Azidoethoxy)-4-bromo-2-fluorobenzene 2-(O(CH2)2N3) B Batch DMF 120 10 69 ± 2 Wang et al117
11 [18F]1-((2-Azidoethoxy)methyl)-4-bromo-2-fluorobenzene 2-(CH2 O(CH2)2N3) B Batch DMF 120 10 90 ± 2 Wang et al117

Abbreviations: DMF, dimethylformamide; DMSO, dimethyl sulfoxide; MR, microreactor (microfluidic); ns, not specified.

a

a

b

Values in plain type are yields before isolation. Values in bold and parentheses are yields after isolation.

c

Uncorrected for decay.

d

Process is 2 steps. Data are for the radiofluorination step.