Precursor
33 (0.7 mg, 2.3
μmol) was dissolved in DMF (80
μL). Tetra-
n-butylammonium hydroxide (TBAH) in MeOH (0.5 M, 4.0
μL) was added to this solution and then injected into the loop of an
AutoLoop apparatus (Bioscan; Washington, DC). [
11C]Iodomethane was released from the PETtrace module and into the loop, which was then kept at room temperature for 5 min. [
11C]
5 was isolated with reversed phase HPLC on a
Luna C18 column (10 × 250 mm, 10
μm; Phenomenex) eluted isocratically with MeCN−10 mM aq HCOONH
4 (45:55 v/v) at 6 mL/min (
tR = 14 min) (see the
Supporting Information). After removal of mobile phase, [
11C]
5 was formulated for intravenous injection in sterile ethanol-saline (10:90 v/v), and sterile-filtered (Millex-MP 0.22
μm, 25 mm; Merck Millipore; Burlington, MA). The identity of the [
11C]
5 was confirmed with reversed phase HPLC on a
Luna C18 column (4.6 mm × 250 mm, 10
μm; Phenomenex) eluted isocratically with MeCN−10 mM aq HCOONH
4 (55:45 v/v) at 2 mL/min (
tR = 5.4 min) (see the
Supporting Information), and by LC-MS (ESI) (method 1) of associated carrier [
tR = 4.80 min, (
m/z) [M + H]
+: 312.4]. [
11C] S was obtained in 20 ± 3% yield from [
11C]carbon dioxide in >99% radiochemical purity and with a molar activity of 125 ± 62 GBq/
μmol (
n = 12).
Singh P., Shrestha S., Cortes-Salva M.Y., Jenko K.J., Zoghbi S.S., Morse C.L., Innis R.B, & Pike V.W. (2018). 3-Substituted 1,5-Diaryl-1H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 1: Synthesis and Pharmacology. ACS chemical neuroscience, 9(11), 2610-2619.