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Facile radiolabelling and purification of 2β‐[O‐ 11 CH 3 ]‐carbomethoxy‐3β‐aryltropanes: Radiotracers for the dopamine transporter
Author(s) -
Wilson Alan A.,
Dasilva Jean N.,
Houle Sylvain
Publication year - 1994
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580340809
Subject(s) - chemistry , tropane , dopamine transporter , radiosynthesis , methylation , in vivo , dopamine , high performance liquid chromatography , alkylation , transporter , stereochemistry , chromatography , biochemistry , microbiology and biotechnology , neuroscience , biology , gene , catalysis
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.