Table 3.
Optimization of [18F]FFNP labeling using the mesylate precursor (6)
| Entry | Precursor (mg) | Base (mg) | Solvent (ML) | Temperature (°C) | Incorporation yielda (%) |
||
|---|---|---|---|---|---|---|---|
| 5 min | 10 min | 15 min | |||||
| 1 | 1.8 | K2CO3/K222 0.4/2.8 | MeCN (600) | 50 | 45.8 | 52.8 | / |
| 2 | 1.8 | K2CO3/K222 0.4/2.8 | MeCN (600) | 63 | 64.9 | 65.2 | / |
| 3 | 1.8 | K2CO3/K222 0.6/3.4 | MeCN (600) | 70 | 43.7 | 43.6 | / |
| 4 | 1.8 | K2CO3/K222 0.4/2.8 | MeCN (600) | 70 | 65.1 | 62.5 | / |
| 5 | 1.8 | K2CO3/K222 0.25/1.4 | MeCN (600) | 70 | 46.7 | 45.0 | / |
| 6 | 1.8 | K2CO3/K222 0.25/1.4 | MeCN (300) | 74 | 28 | / | / |
| 7 | 1.8 | K2CO3/K222 0.25/1.4 | MeCN (600) | 80 | 18 | / | / |
| 8 | 1.8 | K2CO3/K222 0.4/2.8 | MeCN (600) | 81 | 14, 29 | / | / |
| 9 | 1.8 | Bu4NOH 3.57 μL/1 M | MeCN (600) | 70 | 7.6 | 7.3 | / |
| 10 | 1.9 | KHCO3/K222 0.41/2.8 | MeCN (500) | 80 | 18.8 (4min) | 24.1 (8min) | 26.9 (105°C/4min) |
a
Determined by radio-TLC (silica/ethyl acetate).