Table 2.
Compound | Scalea | Solvent (H2O/DMSO)b | T (°C) | RCYc (%) |
---|---|---|---|---|
2 | 3 | 0/100 | 75 | 27 ± 4 |
2 | 3 | 50/50 | 75 | 5 ± 4 |
2 | 3 | 95/5 | 75 | 0d |
3 | 3 | 0/100 | 75 | 92 ± 5 |
3 | 3 | 50/50 | 75 | 89 ± 4 |
3 | 3 | 95/5 | 75 | 93 ± 3 |
4 | 3 | 0/100 | RT | 93 ± 6 |
4 | 3 | 0/100 | 75 | >97 |
4 | 3 | 50/50 | RT | 80 ± 8 |
4 | 3 | 50/50 | 75 | >97 |
4 | 3 | 95/5 | RT | 50 ± 5 |
4 | 3 | 95/5 | 75 | 60 ± 6 |
aμmol
bTotal volume: 200 μL
cEach reaction was performed with 2–10 mCi of [18F]F- following the Method I-VI in the Supplementary Information. Non-decay-corrected RCYs determined by radio-HPLC are presented by means ± standard deviations (n = 3)
dThe precursor was not soluble