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. 2022 May 10;15(5):587. doi: 10.3390/ph15050587

Table 2.

Different reducing agents explored for the nitrile reduction of compound [18F]1 into [18F]2.

graphic file with name pharmaceuticals-15-00587-i001.jpg
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.