Table 1. Optimization of Radiolabeling of 18F-AZD9272.
| entry | precursor (mg) | solvent | reaction time (min) | reaction temperature (°C) | yield (%) |
|---|---|---|---|---|---|
| 1 | 2 | acetonitrile | 5 | 75 | 1 |
| 90 | 1 | ||||
| 110 | 3 | ||||
| 15 | 75 | 1 | |||
| 90 | 1 | ||||
| 110 | 5 | ||||
| 30 | 90 | 2 | |||
| 100 | 5 | ||||
| 2 | 2 | DMSO | 5 | 90 | 0 |
| 120 | 1 | ||||
| 135 | 3 | ||||
| 150 | 5 | ||||
| 10 | 90 | 0 | |||
| 120 | 1 | ||||
| 135 | 5 | ||||
| 150 | 5 | ||||
| 15 | 120 | 2 | |||
| 135 | 6 | ||||
| 150 | 23 | ||||
| 165 | 22 | ||||
| 30 | 150 | 23 | |||
| 165 | 23 | ||||
| 3 | 4–6 | DMSO | 15 | 150 | 23 |
| 4 | 2 | DMF | 15 | 125 | 2 |
| 145 | 15 | ||||
| 30 | 125 | 4 | |||
| 145 | 17 | ||||
| 155 | 15 |