Reference : ENANTIOSELECTIVE SYNTHESES OF NCA (S)-L-[BETA-C-11]-4-CHLOROPHENYLALANINE AND (S)-L-(ALP...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
Human health sciences : Radiology, nuclear medicine & imaging
http://hdl.handle.net/2268/5448
ENANTIOSELECTIVE SYNTHESES OF NCA (S)-L-[BETA-C-11]-4-CHLOROPHENYLALANINE AND (S)-L-(ALPHA-METHYL)-[BETA-C-11]-4-CHLOROPHENYLALANINE
English
Plenevaux, Alain mailto [Université de Liège - ULg > > Centre de recherches du cyclotron >]
Al-Darwich, M. J. [> > > >]
Lemaire, Christian mailto [Université de Liège - ULg > > Centre de recherches du cyclotron >]
Delfiore, Guy [> > > >]
Comar, Dominique [> > > >]
1994
Applied Radiation & Isotopes
Pergamon Press
45
3
361-369
Yes (verified by ORBi)
International
0969-8043
Oxford
United Kingdom
[en] The radiolabeling of (S)-L-4-chlorophenylalanine and (S)-L-(alpha-methyl)-4-chlorophenylalanine were realized with carbon-11 at position beta through a radiochemical synthesis relying on the highly enantioselective reaction between 4-chloro[alpha-C-11]benzyl bromide and the lithium enolate of (S)-1-(t-butyloxycarbonyl)-2-(t-butyl)-3-methyl-1,3-imidazolidine-4-one for (S)-L-[beta-C-11]-4-chlorophenylalanine and of (2S,5S)-1-(t-butyloxycarbonyl)-2-(t-butyl)-3,5-dimethyl-1,3-imidazolidin e-4-one for (S)-L-(alpha-methyl)-[beta-C-11]-4-chlorophenylalanine. Quantities of about 25-35 mCi were obtained at the end of synthesis, ready for injection, after hydrolysis and HPLC purification with a radiochemical yield of 19% corrected to EOB within 45 min. The enantiomeric excesses were shown to be greater than or equal to 97% for both molecules without chiral separation. The radiochemical and the chemical purities of the final compounds were greater than or equal to 98% and the specific activity at the end of synthesis ranged between 250-800 mCi/mu mol.
Centre de Recherches du Cyclotron - CRC
Fonds de la Recherche Scientifique (Communauté française de Belgique) - F.R.S.-FNRS
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/5448

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