The preparation of a fluorine-18 labeled orthocarborane for use in the PET imaging of new boron neutron capture therapy agents
- Univ. of Tennessee Medical Center, Knoxville, TN (United States)
This investigation was undertaken to develop a method to radiofluorinate carboranes which are currently being utilized as boron carriers in boron neutron capture therapy (BNCT). F-18 has been used to label the aromatic ring in a BNCT agent currently utilized in clinical trials. The ortho-carborane moiety is boron-rich and is currently being incorporated into a wide variety of promising new BNCT agents [{open_quotes}Current Topics in The Chemistry of Boron{close_quotes}, The Royal Society of Chemistry, London, 1994.] Consequently, the successful labeling of ortho-carborane with F-18 would permit the pharmacokinetic evaluation of new BNCT agents containing the carborane group. Carrier-added, [F-18]F{sub 2} (0.10 mmole, 22.5 mCi, 833 MBq) was added to orthocarborane (0.06 mmole) dissolved in 0.7 mL of chloroform contained in an evacuated reaction flask which had been cooled to -78 {degrees}C. The reaction mixture was allowed to warm to room temperature while stirring for 20 min. The product, 9-fluoro-ortho-carborane (21% radiochemical yield, 4.8 mCi, 178 MBq) was isolated via TKC using silica gel and 20% ethyl acetate in hexane. The product exhibited physical and spectral characteristics identical to an authentic sample. Traces of isomeric fluorinated ortho-carboranes were detected and were easily separable by chromatography.
- OSTI ID:
- 447785
- Report Number(s):
- CONF-960659-; ISSN 0161-5505; TRN: 97:000961-0065
- Journal Information:
- Journal of Nuclear Medicine, Vol. 37, Issue Suppl.5; Conference: 43. annual meeting of the Society of Nuclear Medicine, Denver, CO (United States), 3-6 Jun 1996; Other Information: PBD: May 1996
- Country of Publication:
- United States
- Language:
- English
Similar Records
Synthesis and animal studies of L-para-(/sup 18/F)-fluorophenyl-alanine as probe for in vivo cerebral protein synthesis
High yield synthesis of 6-(18F)fluoro-L-dopa