Table 2.
Different reducing agents explored for the nitrile reduction of compound [18F]1 into [18F]2.
| ||||
|---|---|---|---|---|
| Entry 1 | Reducing Agents | Reaction Conditions | [18F]2 Conversion 2 | Side Products Conversion 2 |
| 1 | LAH (100 µmol) | THF, r.t., 5min | 15% | 85% |
| 2 | LAH (100 µmol) | THF, 50 °C, 5min | 50% | 50% |
| 3 | BH3.THF (200 µmol) | THF, r.t., 15 min | 5% | 91% |
| 4 | BH3.THF (200 µmol) | THF, 65 °C, 5 min | 5% | 91% |
| 5 | H2 (1 atm) | Pd/C (150 µg), MeOH, r.t., 5 min |
0% | 30% |
| 6 | [RuCl2(p-cymene)2] (1.5 µmol) |
DPPP, NaOH 3M iPrOH, 100 °C, 15 min |
10% | - |
| 7 |
NaBH4 (400 µmol),
NiCl2 6H2O (4 µmol) |
MeOH, r.t., 5 min | 42% | 22% |
| 8 | BER (500 mg), NiCl2 6H2O (20 mg) |
MeOH | <5% | - |
1 Experiments were performed at least in duplicate. 2 Conversion rates of [18F]2 and side products were measured by radio-HPLC as the ratio of formed [18F]2 or side products, respectively, over the total radioactivity. Best conditions were highlighted in red.