Convenient gas phase bromination of [11C]methane and production of [11C]methyl triflate

Synthesis and preliminary biological evaluation of [11C]methyl (2-amino-5-(benzylthio)thiazolo[4,5-d]pyrimidin-7-yl)-d-leucinate for the fractalkine receptor (CX3CR1)

“…The hydrolysis of compound 5 in KOH/methanol at room temperature (RT) for 21 h provided the acid precursor 6 in 50% yield. 12,13 in acetonitrile at 80 °C under basic condition (2 N NaOH).…”

“…The preliminary biological evaluation via radioligand [ 11 [ 11 C]CH3OTf was prepared according to a literature procedure. 13 Melting points were determined on a MEL-TEMP II capillary tube apparatus and were uncorrected. 1 H and 13 C NMR spectra were recorded on a Bruker Avance II 500 MHz NMR Fourier transform spectrometer at 500 and 125 MHz, respectively.…”

“…method 13 within 12 min from [ 11 C]CO2 through [ 11 C]CH4 and [ 11 C]CH3Br with silver triflate (AgOTf) column was passed into the reaction vial at RT until radioactivity reached a maximum (2 min), and then the reaction vial was isolated and heated at 80 °C for 3 min. The contents of the reaction vial were diluted with aqueous NaHCO3 (0.1 M, 1 mL).…”

Synthesis of [11C]CX-6258 as a new PET tracer for imaging of Pim kinases in cancer

“…Our system will have much less 12 C carrier-added in comparison with other 'dry' method and 'wet' method. 25 Chemical purity and radiochemical purity were determined by analytical HPLC. 38 The chemical purity of the precursor 5 and reference standard 4a was >93%.…”

“…[29][30][31] The experimental details and characterization data for compounds 1-5 and for the tracer [ 11 C]4a are given. 39 In summary, a multi-step synthetic route with moderate to high yields for the synthesis of the precursor Ndesmethyl-CX-6258, reference standard CX-6258 and target tracer [ 25 Melting points were determined on a MEL-TEMP II capillary tube apparatus and were uncorrected.…”