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Methylation of the thiophene ring using Carbon-11-labelled methyl iodide: formation of 3-[11C]methylthiophene

✍ Scribed by M. Karramkam; S. Demphel; F. Hinnen; C. Trognon; F. Dollé

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
89 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

This paper describes the radiosynthesis of 3‐[^11^C]methylthiophene, chosen as a model reaction for the preparation of heteroaromatic methylthienyl compounds. Labelling was performed from the corresponding lithiothiophene derivative and [^11^C]methyl iodide as the alkylating agent in THF at −78°C. The conditions used were the following: (1) trapping for 2–3 min at −78°C of the [^11^C]methyl iodide in the THF solution containing the freshly prepared 3‐lithiothiophene; (2) Hydrolysis of the reaction mixture by adding 0.5 ml of the HPLC mobile phase and (3) HPLC purification. 3‐[^11^C]Methylthiophene ([^11^C]‐1) was collected in high yield as the unique peak of the HPLC radiochromatogram. Non‐reacted [^11^C]methyl iodide was not present. Typically, 50–60 mCi (1.85–2.22 GBq) of 3‐[^11^C]methylthiophene ([^11^C]‐1) were obtained within 20 min of radiosynthesis (including HPLC purification) with specific radioactivities ranging from 0.6 to 1.0 Ci/μmol (22.2–37.0 GBq/μmol) starting from 180 to 200 mCi (6.66–7.40 GBq) of [^11^C]CO~2~ (10 μA, 10 min (6000 μC) irradiation). Copyright © 2002 John Wiley & Sons, Ltd.

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