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. 2020 Mar 25;56(34):4668–4671. doi: 10.1039/d0cc00449a

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.