Table 1. Radiosynthesis of [18F]CB251 under various conditionsa.
entry | base | solvent | time (min) | temp. (°C) | RCY (%)b |
---|---|---|---|---|---|
1 | nBu4NHCO3 (0.8 equiv.) | CH3CN | 10 | 120 | <1 |
2 | nBu4NHCO3 (0.8 equiv.) | DMSO | 10 | 140 | <1 |
3 | nBu4NHCO3 (0.8 equiv.) | DMF | 10 | 140 | <1 |
4 | nBu4NHCO3 (0.8 equiv.) | tert-BuOH | 10 | 120 | 4.1 ± 1.5b |
5 | nBu4NHCO3 (0.8 equiv.) | tert-BuOH | 30 | 120 | 4.0 ± 1.2b |
6 | nBu4NHCO3 (2.0 equiv.) | tert-BuOH | 10 | 120 | 17.3 ± 4.9b |
7 | nBu4NHCO3 (4.0 equiv.) | tert-BuOH | 10 | 120 | 28.1 ± 7.2c |
8 | nBu4NHCO3 (8.0 equiv.) | tert-BuOH | 10 | 120 | 10.6 ± 4.8b |
9 | K2.2.2/K2CO3 (5 mg/0.8 equiv.) | tert-BuOH | 10 | 120 | 14.7 ± 4.2b |
10 | K2.2.2/K2CO3 (5 mg/2.0 equiv.) | tert-BuOH | 10 | 120 | 1.7 ± 0.5b |
aThe reaction was carried out using different equivalents of base relative to the precursor (3.0 mg) in 0.4 mL of solvent.
bThe radiochemical yield (RCY) was determined by radio-TLC (n = 3).
cn = 21.