[en] Since 1998, routine [18F]FDG syntheses are being carried out by alkaline hydrolysis on a solid support, i.e. the labeled intermediate is trapped on a tC18 solid phase extraction cartridge, purified and finally hydrolyzed within the cartridge, at room temperature, using sodium hydroxide. The present study demonstrated that no epimerization of [18F]FDG to [18F]FDM occurs even when 12 N NaOH is used and when the hydrolysis time is extended up to 1 h. The alkaline hydrolysis on solid support appears to be a simple method leading to [18F]FDG with high purity.
Disciplines :
Energy Radiology, nuclear medicine & imaging Chemistry
Author, co-author :
Mosdzianowski, C.
Lemaire, Christian ; Université de Liège - ULiège > Centre de recherches du cyclotron
Simoens, F.
Aerts, Joël ; Université de Liège - ULiège > Centre de recherches du cyclotron
Morelle, J. L.
Luxen, André ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron
Language :
English
Title :
Epimerization study on [18F]FDG produced by an alkaline hydrolysis on solid support under stringent conditions
Publication date :
June 2002
Journal title :
Applied Radiation and Isotopes
ISSN :
0969-8043
Publisher :
Pergamon-Elsevier Science Ltd, Oxford, United Kingdom
Füchtner F., Steinbach J., Mäding P., Johannsen B. (1996) Basic hydrolysis 2-[18F]Fluoro-1,3,4,6-tetra-O-acetyl-D-glucose in the preparation of 2-[18F]Fluoro-2-deoxy-D-glucose. Appl. Radiat. Isot. 47(1):61-66.
Hamacher K., Coenen H.H., Stöcklin G. (1986) Efficient stereospecific synthesis of no-carrier-added 2-[18F]Fluoro-2-Deoxy-D-glucose using aminopolyether supported nucleophilic substitution. J. Nucl. Med. 27:235-238.
Lemaire C., Damhaut Ph., Lauricella B., Morelle J.-L., Monclus M., Van Naemen J., Mulleneers E., Aerts J., Plenevaux A., Brihaye C., Luxen A. (1997) Synthesis of [18F]FDG with alkaline hydrolysis on a low polarity solid phase support. J. Label. Compd. Radiopharm. 40:256-257.
Lemaire C., Damhaut Ph., Lauricella B., Mosdzianowski C., Morelle J.-L., Monclus M., Van Naemen J., Mulleneers E., Aerts J., Plenevaux A., Brihaye C., Luxen A. Fast [18F]FDG synthesis by alkaline hydrolysis on a low polarity solid phase support. J. Label. Compd. Radiopharm., submitted for publication; .
Meyer G.-J., Matzke K.H., Hamacher K., Füchtner F., Steinbach J., Notohamiprodjo G., Zijlstra S. (1999) The stability of 2-[18F]Fluoro-Deoxy-D-glucose towards epimerisation under alkaline conditions. Appl. Radiat. Isot. 51:37-41.
Mosdzianowski C., Lemaire C., Lauricella B., Aerts J., Morelle J.-L., Gobert F., Herman M., Luxen A. (1999) Routine and multi-curie level productions of [18F]FDG using an alkaline hydrolysis on solid support. J. Label. Compd. Radiopharm. 42:515-516.
Mulhholland G.K. (1995) Simple rapid hydrolysis of acetyl protecting groups in the FDG synthesis using cation exchange resins. Nucl. Med. Biol. 22(1):19-23.
Varelis P., Barnes R.K. (1996) Epimerization of 2-Deoxy-2-[18F]Fluoro-D-glucose under basic conditions. A convenient method for the preparation of 2-Deoxy-2-[18F]Fluoro-D-mannose. Appl. Radiat. Isot. 47(8):731-733.
Wienhard K., Pawlik G., Nebeling B., Rudolf J., Fink G., Hamacher K., Stöcklin G., Heiss W.-D. (1991) Estimation of local cerebral glucose utilization by positron emission tomography: Comparison of [18F]2-Fluoro-2-Deoxy-D-Glucose and [18F]2-Fluoro-2-Deoxy-D-mannose in patients with focal brain lesions. J. Cereb. Blood Flow Metab. 11:485-491.