Table 1.
entrya | temp (°C) | time (min) | proton source | proton source (μL)b | yield ratio of [18F]PS13 to [18F]5c | yield of [18F]PS13c (%) | Am of [18F]PS13d (GBq/μmol) |
---|---|---|---|---|---|---|---|
1 | 90 | 20 | IPA | 10.8 | 1:5 | ||
2e | 90 | 20 | IPA | 21.6 | 1:2.5 | ||
3 | 90 | 20 | tert-BuOH | 21.6 | 1:5 | ||
4 | 130 | 20 | IPA | 21.6 | 1:2 | ||
5 | 130 (MW) | 20 | IPA | 21.6 | 1:2.5 | ||
6 | 130 | 2 | (NH4)2CO3(aq.) | 1.6 | 1:5 | ||
7f | 130 | 20 | NH4Cl(aq.) | 1.6 | 1:0.9 | 0.8 | 14.2 |
8e | 130 | 20 | NH4Cl(aq.) | 3.2 | 1:0.4 | 3.3 | 16.8 |
9 | 130 | 20 | NH4Cl(aq.) | 6.4 | 1:0.4 | 0.8 | 8.6 |
10 | 130 | 20 | NH4Cl(aq.) | 16 | 0:0 | 0 | |
11 | 130 (MW) | 2 | NH4Cl(aq.) | 1.6 | 1:10 | ||
12g | 130 | 20 | IPA | 21.6 | 5.9 | 0.6 | |
13g | 130 | 10 | IPA | 21.6 | 4.5 | 1.0 |
Reactions (n = 1) were performed with 5 (1.5 mg) in DMSO (300 μL), unless otherwise noted.
Volume per reaction.
Yield ratios and yields were determined from radiochromatograms acquired during HPLC analysis of the crude reaction mixture.
Decay-corrected to ERP.
n = 2.
n = 4.
Reaction used 3 mg of precursor 5.