Precursor synthesis and radiolabelling of the dopamine D-2 receptor ligand [C-11]raclopride from [C-11]methyl triflate

Desmethyl-raclopride was synthesized via a straightforward, three-step synthetic approach and used for the preparation of [C-11]raclopride from [C-11]methy] triflate. Conditions for the radiolabelling were optimized to obtain a simple and reproducible procedure suitable for automation. [C-11]Raclopr...

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Bibliographic Details
Published inJournal of labelled compounds & radiopharmaceuticals Vol. 42; no. 12; pp. 1183 - 1193
Main Authors Langer, O, Nagren, K, Dolle, F, Lundkvist, C, Sandell, J, Swahn, CG, Vaufrey, F, Crouzel, C, Maziere, B, Halldin, C
Format Journal Article
LanguageEnglish
Published W SUSSEX Wiley 1999
Subjects
Biochemical Research Methods
Biochemistry & Molecular Biology
Chemistry
Chemistry, Analytical
Chemistry, Medicinal
Life Sciences & Biomedicine
Medicin och hälsovetenskap
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
DRUG
PET RADIOLIGANDS
[C-11]methyl triflate
[C-11]raclopride
IODIDE
HIGH-AFFINITY
dopamine D-2 receptor antagonist
BETA-CIT
BINDING
C-11 METHYL TRIFLATE
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Summary:Desmethyl-raclopride was synthesized via a straightforward, three-step synthetic approach and used for the preparation of [C-11]raclopride from [C-11]methy] triflate. Conditions for the radiolabelling were optimized to obtain a simple and reproducible procedure suitable for automation. [C-11]Raclopride was prepared with an average radiochemical yield of 55-65% (decay corrected, based on starting [C-11]methyl triflate) in a total synthesis time (including purification and formulation of product) of 35 min. The radiolabelling procedure used significantly less precursor, avoided the use of DMSO, and was shorter compared to the standard radiolabelling procedure with [C-11]methyl iodide.
ISSN:0362-4803