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. 2022 Jan 28;15(2):162. doi: 10.3390/ph15020162

Table 1.

Optimization of the reaction parameters for copper-mediated radiofluorination of (S)-35.

Entry (S)-35 (µmol) Cu Complex Eq. Cu Complex 1 Eq. of Pyrizdine 1 RCY 2 (%)
1 10 Cu(OTf)2 2 15 5
2 10 Cu(OTf)2 4 15 28
3 20 Cu(OTf)2 2 2.5 7
4 20 Cu(OTf)2 2 4 30
5 20 Cu(OTf)2 2 5 31
6 20 Cu(OTf)2 2 7.5 24
7 20 Cu(OTf)2 2 15 11
8 20 Cu(OTf)2 2 25 9
9 20 Cu(OTf)2 4 5 15
10 20 Cu(OTf)2 4 7.5 18
11 20 Cu(OTf)2 4 15 12
12 20 Cu(OTf)2 4 25 5
13 30 Cu(OTf)2 2 5 27
14 30 Cu(OTf)2 4 15 12
15 20 Cu(OTf)2(py)4 1 0 37
16 20 Cu(OTf)2(py)4 1.5 0 54
17 20 Cu(OTf)2(py)4 2 0 41
18 20 Cu(OTf)2(py)4 2.5 0 36

1 related to the molar amount of precursor. 2 determined by radio-TLC analyses of the crude reaction mixture after 10 min of reaction time at 110 °C.