Table 2. Reaction conditions and optimisation for the synthesis of [11C]1 using BEMP as a trapping agent (see footnote ‡).
Entry a | KF (eq.) | K2.2.2 (eq.) | BEMP (eq.) | CuI (%) | TE (%) | RCY [11C]1 (%) |
1 b | 0.25 | 0.25 | 0.6 | 10 | 84 ± 3 | 33 ± 15 |
2 | 0.25 | 0.25 | 0.6 | 10 | 89 ± 8 | 93 ± 6 |
3 c | 0.25 | 0.25 | 0.6 | 10 | 76 ± 12 | 58 ± 9 |
4 | 0.25 | 0.25 | — | 10 | 6 ± 2 | 95 ± 1 |
5 | 0.25 | 0.25 | 0.6 | — | 76 ± 22 | 24 ± 18 |
6 d | — | 0.25 | 0.6 | 10 | 40, 30 | 0 |
7 e | 0.25 | — | 0.6 | 10 | 48 | 0 |
8 f | 0.125 | 0.125 | 0.6 | 10 | 55 ± 15 | 47 ± 9 |
9 g | 0.25 | 0.25 | 0.6 | 10 | 12 ± 5 | 20 ± 7 |
10 e , h | 0.25 | 0.25 | 0.6 | 10 | 50 | 0 |
a n = 3.
b100 °C.
c2.5 minutes.
d n = 2.
e n = 1.
f 1a (50 μmol).
gTHF.
hMeCN.