Synthesis of ¹¹C‐labelled acamprosate for PET studies

Abstract

SummaryA method for labelling acamprosate (calcium N-acetyl homotaurinate), an anti-craving compound for ethanol, with 11

Reliable set-up for in-loop 11C-carboxylations using Grignard reactions for the preparation of [carbonyl-11C]WAY-100635 and [11C]-(+)-PHNO

“…Comparing the published data, all procedures lead to a suitable reaction outcome for further use, but specific radioactivities achieved by loop-methods are superior to those in “wet” methods. In-loop reactions for carbon-11-labeled radioligands have been described for both 11 C-methylations ( Gómez et al, 2008; Wilson et al, 2000, 2009; Iwata et al 2001 ) and 11 C-carboxylations using Grignard reactions ( Arai et al, 2009; Courtyn et al, 2001; Krasikova et al, 2003; Luthra et al, 1990; Matarrese et al, 2002; McCarron et al, 1996; Zhang et al, 2006 ). We previously published an in-loop set-up for the routine production of [ carbonyl - 11 C]WAY-100635 ( Wadsak et al, 2007 ) which is still in use in our facility in various clinical studies dealing with the (patho-)physiological distribution of serotonin 5HT 1A receptor, e.g.…”

Synthesis of a 11C‐labelled taxane derivative by [1‐11C]acetylation

“…The synthesis of 6 is described in literature using different Grignard reagents before addition of phthaloyl dichloride: MeMgBr in diethylether, 6 MeMgBr in THF, 7 MeMgCl or MeLi in diethylether 8 and MeMgCl in THF. 9 We have tested the several Grignard/ solvent combinations and found out, that only the use of MeMgBr in diethylether 6 gave a radiochemical pure 6. The other combinations caused a non-identified radioactive by-product of up to 50%.…”

State of Art in 11C Labelled Radiotracers Synthesis

“…The increased medical use of paclitaxel has resulted in a number of biological questions including : determination of adequate dosing regime, therapeutic tissue concentration, cellular/intracellular accumulation and resistance to treatment [269] availability of a suitable radiolabelled ligand for these sites may help begin answering some of these biological questions. The increased medical use of paclitaxel has resulted in a number of biological questions including : determination of adequate dosing regime, therapeutic tissue concentration, cellular/intracellular accumulation and resistance to treatment [269] availability of a suitable radiolabelled ligand for these sites may help begin answering some of these biological questions.…”

“…The labelling was performed using [ 11 C]acetyl chloride [269] (Fig. It is suggested that acamprosate acts by reducing neuronal hyperexcitability.…”