✦ LIBER ✦

Facile radiolabelling and purification of 2β-[O-11CH3]-carbomethoxy-3β-aryltropanes: Radiotracers for the dopamine transporter

✍ Scribed by Alan A. Wilson; Jean N. Dasilva; Sylvain Houle

Publisher: John Wiley and Sons
Year: 1994
Tongue: French
Weight: 350 KB
Volume: 34
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580340809

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✦ Synopsis

Abstract

Two potent dopamine transporter ligands, 2β‐[O‐^11^CH~3~]‐carbomethoxy‐3β‐(4‐methylphenyl)tropane and its 4‐chlorophenyl analogue, were synthesized by O‐alkylation at the 2β‐carboxy position with [^11^C]‐iodomethane. Separation of the [^11^C]‐labelled tropane from excess carboxylic acid precursor was readily achieved by semipreparative HPLC providing pure radiotracers at high specific activities (800–3000 mCi/μmole) suitable for in vivo PET studies. Radiosynthesis of this class of compounds by [O‐^11^CH~3~]‐methylation offers advantages over previously reported [N‐^11^CH~3~]‐methylation methods.

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