Synthesis of 4-dihydroxyboryl-2-[18F]fluorophenylalanine with relatively high-specific activity

An alternative procedure to produce 4‐dihydroxyboryl‐2‐[18F]fluorophenylalanine ([18F]FBPA) for positron emission tomography studies in boron neutron capture therapy is described. Relatively high‐specific activity electrophilic radiofluorine is produced using a post‐target conversion of [18F]F– to [...

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Veröffentlicht in:	Journal of labelled compounds & radiopharmaceuticals 2002-07, Vol.45 (8), p.697-704
Hauptverfasser:	Vähätalo, Jyrki K., Eskola, Olli, Bergman, Jörgen, Forsback, Sarita, Lehikoinen, Pertti, Jääskeläinen, Juha, Solin, Olof
Format:	Artikel
Sprache:	eng
Schlagworte:	4-dihydroxyborylphenylalanine Aliphatic compounds Biological and medical sciences boron neutron capture therapy Chemistry Contrast media. Radiopharmaceuticals electrophilic fluorine Exact sciences and technology LC-MS Medical sciences Organic chemistry Pharmacology. Drug treatments Preparations and properties specific radioactivity
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Zusammenfassung:	An alternative procedure to produce 4‐dihydroxyboryl‐2‐[18F]fluorophenylalanine ([18F]FBPA) for positron emission tomography studies in boron neutron capture therapy is described. Relatively high‐specific activity electrophilic radiofluorine is produced using a post‐target conversion of [18F]F– to [18F]F2. Liquid chromatography with mass spectrometric detection is used to estimate the specific radioactivity of [18F]FBPA and to verify the quality control for chemical identity of the target compound. [18F]FBPA produced according to this method fulfilled the pharmaceutical quality requirements for an injection in patients. Copyright © 2002 John Wiley & Sons, Ltd.
ISSN:	0362-4803 1099-1344
DOI:	10.1002/jlcr.600