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

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.