Table 1.
Entry | Conditions
|
Solvent | TEMPO (eq.) | [18F]F− incorporation (%)
|
|||
---|---|---|---|---|---|---|---|
Energy source | Temp. (°C) | Time (min) | Putative [18F]16 | [18F]11 | |||
1 | Thermal | 100 | 5 | DMF | -- | 26 | 0 |
2 | Thermal | 100 | 5 | DMF | 2 | 39 | 3 |
3 | μ-wave 100 W | 60–140 | 2 | DMF | 2 | 40 | 11 |
4 | μ-wave 90 W | 61–113 | 2.5 | MeCN | 4 | 30 | 0 |
5 | μ-wave 90 W | 60–149 | 2 | DMSO | 2 | 9 | 40 |
6 | μ-wave 90 W | 60–152 | 4 | DMSO | 2 | 3 | 29 |
7 | μ-wave 90 W | 60–149 | 2 | DMSO | 2 | n.m. | 18 (n = 2)b |
8 | μ-wave 90 W | 60–152 | 2.5 | DMSO | 2 | 0–14 | 38 (n =13)b |
Amounts of precursor were 1.4–1.9 mg, and reaction volume was 500 μL.
Products from reactions 7 and 8 were analyzed on a semi-preparative HPLC column, whereas other reactions were analyzed on an analytical column.
n.m. = not measured