Table 1. Optimization of the Reaction Conditionsa.
entry | deviation from standard conditions | RCY (%) |
---|---|---|
1 | none | 46 ± 14n=4 |
2 | DMF as solvent | 44n=1 |
3 | CHCl3 as solvent | 40 n=1 |
4 | 50 °C instead of 80 °C | 27n=1 |
5 | 9 μmol PhIO | 16n=1 |
6 | 36 μmol PhIO | 49n=1 |
7 | 1 μmol 3 | 32n=1 |
8 | 4 μmol 3 | 26n=1 |
[18F]TEAF was prepared with a NEt4HCO3 (9 mg) elution protocol. Bz: benzoyl. RCY: radiochemical yield, determined by radioHPLC analysis of the crude reaction mixture.