Table 1. Reaction conditions and optimisation for the synthesis of [11C]1 using DBU as a trapping agent (see footnote ‡).
Entry a | Fluoride source (eq.) | Additive (eq.) | DBU (eq.) | CuI (%) | TE (%) | RCY [11C]1 (%) |
1 b | CsF (3) | 18-Crown-6 (3) | — | — | 6 | 0 |
2 b | CsF (3) | 18-Crown-6 (3) | — | 10 | 99 | 0 |
3 b | CsF (3) | 18-Crown-6 (3) | 0.6 | 10 | 77 | 0 |
4 b | KF (3) | K2.2.2 (3) | 0.6 | 10 | 96 | 21 |
5 | KF (0.5) | K2.2.2 (0.5) | 0.6 | 10 | 63 ± 14 | 41 ± 9 |
6 | KF (0.25) | K2.2.2 (0.25) | 0.6 | 10 | 52 ± 5 | 53 ± 23 |
7 a , c | KF (0.5) | K2.2.2 (0.5) | 0.6 | 10 | 77 | 40 |
8 c | KF (0.25) | K2.2.2 (0.25) | 0.6 | 10 | 67 ± 13 | 55 ± 7 |
9 b , d | KF (0.25) | K2.2.2 (0.25) | 0.6 | 10 | 37 | 0 |
10 | KF (0.25) | K2.2.2 (0.25) | 0.9 | 10 | 86 ± 5 | 28 ± 11 |
11 | KF (0.25) | K2.2.2 (0.25) | 0.6 | 20 | 61 ± 31 | 44 ± 26 |
12 b , c , e | KF (0.25) | K2.2.2 (0.25) | 0.6 | 10 | 7 | 15 |
a n = 3.
b n = 1.
c140 °C.
d70 °C.
eTHF.