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Synthesis of two dopamine D4 receptor ligands: 11 C labelled chromeno[3,4‐c]pyridin‐5‐ones
Author(s) -
De Vos F.,
Dumont F.,
Santens P.,
Slegers G.,
Dierckx R. A.,
De Reuck J.
Publication year - 2000
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 - 10.1002/1099-1344(200009)43:10<989::aid-jlcr384>3.0.co;2-3
Subject(s) - chemistry , high performance liquid chromatography , desmethyl , specific activity , dopamine , tetrabutylammonium hydroxide , tracer , hydroxide , methylation , radiochemistry , chromatography , organic chemistry , enzyme , metabolite , biochemistry , physics , neuroscience , nuclear physics , gene , biology
The synthesis of two 11 C labelled chromeno[3,4‐c]pyridin‐5‐ones for the visualisation of the dopamine D4 receptor subtype has been developed. The production entailed an O ‐methylation of the O ‐desmethyl precursor with [ 11 C]iodomethane in the presence of tetrabutylammonium hydroxide. Subsequent purification by RP‐HPLC and formulation by tracer enrichment on a C18 Sep Pak provided a solution which was suitable for human iv injection. Specific activity of the tracer averaged 37 GBq/μmol at EOS and the radiochemical yields were 65% (decay‐corrected, based on [ 11 C]CH 3 I). Total activity obtained was 5·6–7·4 GBq. The preparations have been demonstrated to be chemically and radiochemically pure by HPLC. Copyright © 2000 John Wiley & Sons, Ltd.