Time-efficient and convenient synthesis of [ 18F]altanserin for human PET imaging by a new work-up procedure
[ 18F]Altanserin, an important PET radioligand for the in vivo imaging of the 5-HT 2A receptor, was synthesized from its precursor nitro-altanserin in DMF or DMSO at high temperatures of 150 °C in an overall radiochemical yield (EOB) of 23–25% after 75 min. A new solid phase work-up procedure involv...
Gespeichert in:
Veröffentlicht in: | Applied radiation and isotopes 2009-11, Vol.67 (11), p.2040-2043 |
---|---|
Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | [
18F]Altanserin, an important PET radioligand for the
in vivo imaging of the 5-HT
2A receptor, was synthesized from its precursor nitro-altanserin in DMF or DMSO at high temperatures of 150
°C in an overall radiochemical yield (EOB) of 23–25% after 75
min. A new solid phase work-up procedure involving the acidification of the crude reaction mixture and a C18-SepPak-solid phase separation preceded the final HPLC purification. This led to a significantly reduced synthesis time as a result of a stable and early elution from the HPLC column using improved HPLC conditions (MeOH/THF/NaOAc 0.05
N pH 5: 27/18/55, flow: 5
mL/min, Symetry Prep 7
μm C18 (Waters)). The synthesis was performed semi-automatically in a modified GE TracerLab synthesis module using an in-house-developed program. The synthesized [
18F]altanserin was used in our ongoing human and animal PET imaging studies. |
---|---|
ISSN: | 0969-8043 1872-9800 |
DOI: | 10.1016/j.apradiso.2009.07.020 |