Table 1.
Radiochemical yields of [18F]fluoroarenes from the microfluidic NCA radiofluorination of diaryliodonium tosylates (XC6H4I+C6H4Y TsO−; 9.5 mM) in DMF-0.25% H2O containing K 2.2.2-K2CO3 at 150 °C for 181 s.
XC6H4I+C6H4Y TsO−
|
Radioactivity recoverya (%) | RCY (%)b
|
||||
---|---|---|---|---|---|---|
# | X | Y | [18F]FC6H4X | [18F]FC6H4Y | ||
1 | H | H | 96 | 49 | ||
2 | H | 2-Me | 61 | 7 | 16 | |
3 | H | 2-Br | 87 | 0 | 14 | |
4 | 4-OMe | 2-CN | 92 | 0 | 96 | |
5 | 4-OMe | 4-CO2Me | 100 | 0 | 90 | |
6 | 4-OMe | 4-CN | 100 | 0 | 83 | |
7 | 4-OMe | 2-Me | 75 | 0 | 66 | |
8 | 4-OMe | 4-COC6H4-4′-Br | 80 | 0 | 49 | |
9 | 4-OMe | 3-CO2Et | 100 | 0 | 37 | |
10 | 4-OMe | 3-CF3 | 100 | 0 | 29 | |
11 | 4-OMe | 3-NO2 | 100 | 0 | 17 | |
12 | 4-OMe | 4-Ph | 56 | 0 | 16 | |
13 | 4-OMe | 3-CN | 73 | 4 | 11 | |
14 | 4-OMe | 4-F | 97 | 0 | 13 | |
15 | 4-OMe | 4-OMe | 92 | 12 |
% of infused radioactivity collected from the microfluidic apparatus at end of reaction.
Radiochemical yield measured by radio-HPLC as an average from two experiments.