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High Molar Activity of [11C]TCH346 via [11C]methyl Triflate Using the "Wet" [11C]CO2 Reduction Method

High Molar Activity of [11C]TCH346 via [11C]methyl Triflate Using the "Wet" [11C]CO2 Reduction Method

Johannes Ermert, Stefan Stüsgen, Markus Lang, Werner Roden, Heinz H Coenen

Appl Radiat Isot. 2008 May;66(5):619-24.

PMID: 17827025

Abstract:

[(11)C]TCH346, a compound acting on the glycolytic enzyme, glycerol-aldehyde-3-phosphate dehydrogenase, was produced under optimised conditions by methylation of the desmethyl compound with no-carrier added (n.c.a.) [(11)C]methyl triflate. An i.v. injectable solution of n.c.a. [(11)C]TCH346 containing 4040+/-1550 MBq (n=6) containing a molar activity between 40 and 5700 GBq/micromol and a radiochemical purity of >99% was obtained within 30 min (after EOB) by irradiation of nitrogen gas containing 0.5% oxygen with 16.5 MeV protons at 45 microA for 30 min. The alkylation reagent [(11)C]methyl triflate was prepared via on-line conversion of [(11)C]methyl iodide. For the formation of [(11)C]methyl iodide, [(11)C]carbon dioxide from the target chamber was reduced by a lithium aluminium hydride solution, and the methanol obtained on-line was converted using triphenylphosphine diiodide. The molar activity of [(11)C]TCH346 could be improved from 40 up to nearly 5700GB q/micromol during the optimisation of the synthesis using the same stock solution of lithium aluminium hydride solution in tetrahydrofuran.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP77299639	Lithium diisobutyl-tert-butoxyaluminum hydride solution		77299-63-9	Price

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