Journal of labelled compounds and radiopharmaceuticals p. 1289 - 1300 (1999)
Update date:2022-07-30
Topics:
Gilissen
Bormans
De Groot
Verbruggen
We have prepared two radiolabelled analogues of hemicholinium-3 (HC-3) as potential in vivo tracers of the sodium dependent high affinity choline uptake (SDHAChU) system. Thus, 4-[1-hydroxy-2-(4-[18F]fluoromethylpiperidinyl)ethyl]-4'-[1-hydroxy-2-(4 -methylpiperidinyl)ethyl]biphenyl ([18F]FA-4) and 4-[1-hydroxy-2-(4-11C]methylpiperazinyl)ethyl]-4'-[1-hydroxy-2-(4 -methylpiperidinyl)]biphenyl ([11C]pipzA-4) have been synthesized. [18F]FA-4 was prepared by reaction of 4-[18F]fluoromethylpiperidine with 4-(α-bromoacetyl)-4'-(4-methylpiperidinylacetyl)biphenyl followed by reduction of the keto groups to alcohols with NaBH4. The total synthesis time was 300 minutes and [18F]FA-4 was obtained with a specific activity of 5.6 GBq/μmol (EOS) and an overall decay corrected radiochemical yield of 3.1 ± 0.6%. [11C]pipzA-4 was prepared by reaction of [11C]methyl triflate with 4-[1-hydroxy-2-piperazinyl)ethyl]-4'-[1-hydroxy-2-(4 -methylpiperidinyl)ethyl]biphenyl. The total synthesis time was 25 minutes and [11C]pipzA-4 was obtained with a specific activity of 13.7 GBq/μmol (EOS) and an overall decay corrected radiochemical yield of 19.5 ± 2.2%.
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