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Influence of the electron rich (hetero)aryl Arb on the radiochemical yield and regioselectivity of radiohalogenation of 4a–c (n ≥ 3).
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|---|---|---|---|---|
| Iodonium | 125I | 211At | ||
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| % (I)a | % (II) | % (I)a | % (II) | |
| 4a | 36 ± 5 | 2 ± 1 | 90 ± 2 | 6 ± 1 |
| 4b | 50 ± 3 | 1 ± 1 | 85 ± 3 | 6 ± 1 |
| 4c | 87 ± 1 | 1 ± 1 | 79 ± 2 | 12 ± 1 |
1–3% of total activity of the reaction mixture contained also the carboxylic acid form of I due to hydrolysis of the N-hydroxysuccinimidyl ester.
