Simple synthesis of new carbon-11-labeled 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives for PET imaging of A sub(3) adenosine receptor

Simple synthesis of new carbon-11-labeled 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives for PET imaging of A sub(3) adenosine receptor

The reference standards 4a-b, 6a-b, 7a-c, and desmethylated precursors 9a-b, 10a-b, 8a-c were synthesized from 4-methoxyaniline, ethyl 2-chloro-acetoacetate and substituted benzene-1,2-diamines with 3, 5, 6 steps in 61-67%, 34-41%, 23-31%, and with 4, 6, 7 steps in 49-57%, 28-35%, 20-27% overall che...

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Veröffentlicht in:Applied radiation and isotopes 2014-09, Vol.91, p.71-78
Hauptverfasser: Gao, Mingzhang, Gao, Andy Chufan, Wang, Min, Zheng, Qi-Huang
Format: Artikel
Sprache:eng
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Zusammenfassung:The reference standards 4a-b, 6a-b, 7a-c, and desmethylated precursors 9a-b, 10a-b, 8a-c were synthesized from 4-methoxyaniline, ethyl 2-chloro-acetoacetate and substituted benzene-1,2-diamines with 3, 5, 6 steps in 61-67%, 34-41%, 23-31%, and with 4, 6, 7 steps in 49-57%, 28-35%, 20-27% overall chemical yield, respectively. The target tracers [ super(11)C]4a-b, [ super(11)C]6a-b, [ super(11)C]7a-c were synthesized from their corresponding precursors with [ super(11)C]CH sub(3)OTf through O-[ super(11)C]methylation and isolated by simplified SPE in 40-60% decay corrected radiochemical yields at EOB, with 185-370 GBq/ mu mol specific activity at EOS.
ISSN:0969-8043
DOI:10.1016/j.apradiso.2014.05.005