Fully automated radiosynthesis of both enantiomers of [18F]Flubatine under GMP conditions for human application

Marianne Patt; Andreas Schildan; Bernd Habermann; Steffen Fischer; Achim Hiller; Winnie Deuther-Conrad; Stephan Wilke; René Smits; Alexander Hoepping; Gudrun Wagenknecht; Jörg Steinbach; Peter Brust; Osama Sabri

doi:10.1016/j.apradiso.2013.05.009

Fully automated radiosynthesis of both enantiomers of [18F]Flubatine under GMP conditions for human application

Appl Radiat Isot. 2013 Oct:80:7-11. doi: 10.1016/j.apradiso.2013.05.009. Epub 2013 Jun 7.

Authors

Marianne Patt¹, Andreas Schildan, Bernd Habermann, Steffen Fischer, Achim Hiller, Winnie Deuther-Conrad, Stephan Wilke, René Smits, Alexander Hoepping, Gudrun Wagenknecht, Jörg Steinbach, Peter Brust, Osama Sabri

Affiliation

¹ Department of Nuclear Medicine, University of Leipzig, Liebigstrasse 18, D-04103 Leipzig, Germany. [email protected]

PMID: 23792828
DOI: 10.1016/j.apradiso.2013.05.009

Abstract

A fully automatized radiosynthesis of (+)- and (-)-[(18)F]Flubatine ((+)- and (-)NCFHEB) by means of a commercially available synthesis module (TRACERlab FX FN) under GMP conditions is reported. Radiochemical yields of 30% within an overall synthesis time of 40 min were achieved in more than 70 individual syntheses. Specific activities were approximately 3000 GBq/μmol and radiochemical purity was determined to be at least 97%.

Keywords: Automation; Flubatine; Fluorine-18; GMP; NCFHEB; α(4)β(2) Nicotinic acetylcholine receptors.

MeSH terms

Automation*
Benzamides / chemical synthesis*
Benzamides / chemistry
Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
Bridged Bicyclo Compounds, Heterocyclic / chemistry
Chromatography, High Pressure Liquid
Fluorine Radioisotopes / chemistry*
Humans
Quality Control
Stereoisomerism

Substances

Benzamides
Bridged Bicyclo Compounds, Heterocyclic
Fluorine Radioisotopes
fluoronorchloroepibatidine