Preliminary investigation of the 125I-iodination and 211At-astatination of 4-chlorobenzeneboronic acid (1). RCYs determined by radio-HPLC analysis of the crude producta.
| |||||
|---|---|---|---|---|---|
| C(1) (mM) | C(Cu(OTf)2pyr4) (mM) | C(1,10-phenanthroline) (mM) | Solvent (v : v) | RCY (%)a | |
| 125I | 211At | ||||
| 25 | 0 | 0 | MeOH/H2O (9 : 1) | 0 | 44 ± 7b |
| 25 | 25 | 0 | MeOH/H2O (9 : 1) | 99 ± 1 | 99 ± 1 |
| 10 | 10 | 0 | MeOH/H2O (9 : 1) | >99 | 98 ± 3 |
| 0.25 | 10 | 0 | MeOH/H2O (9 : 1) | >99 | 99 ± 1 |
| 0.25 | 10 | 0 | H2O/MeOH (85 : 15) | 17 ± 2 | 74 ± 5 |
| 0.25 | 0 | 0 | H2O/MeOH (85 : 15) | — | 0 |
| 0.25 | 10 | 10 | H2O/MeOH (85 : 15) | 85 ± 2 | >99 |
| 0.25 | 10 | 10 | H2O/DMF (85 : 15) | 91 ± 1 | 99 ± 1 |
| 0.25 | 10 | 10 | H2O/DMSO (85 : 15) | 88 ± 2 | 99 ± 1 |
a
Standard conditions : [125I]NaI or [211At]NaAt (0.5–1 MBq), 100 μL, 30 min, 23 °C, average of n = 3 runs.
b
n = 7.