78756-03-3Relevant articles and documents
Facile aromatic radiofluorination of [18F]flumazenil from diaryliodonium salts with evaluation of their stability and selectivity
Moon, Byung Seok,Kil, Hee Seup,Park, Jun Hyung,Kim, Ji Sun,Park, Jimin,Chi, Dae Yoon,Lee, Byung Chul,Kim, Sang Eun
, p. 8346 - 8355 (2012/05/04)
Aromatic radiofluorination of the diaryliodonium tosylate precursor with [18F]fluoride ions has been applied successfully to access [ 18F]flumazenil in high radiochemical yields of 67.2 ± 2.7% (decay corrected). The stability and reactivity of the diaryliodonium tosylate precursor plays a key role in increasing the production of 18F- labelled molecules under the fluorine-18 labelling condition. Various conditions were explored for the preparation of [18F]flumazenil from different diaryliodonium tosylate precursors. Optimum incorporation of [ 18F]fluoride ions in the 4-methylphenyl-mazenil iodonium tosylate precursor (5f) was achieved at 150°C for 5 min by utilizing 4 mg of the precursor, K2.2.2/K2CO3 complex, and the radical scavenger in N,N-dimethylformamide. This approach was extended to a viable method for use in automated synthesis with a radiochemical yield of 63.5 ± 3.2% (decay corrected, n = 26) within 60.0 ± 1.1 min. [ 18F]Flumazenil was isolated by preparative HPLC after the reaction was conducted under improved conditions and exhibited sufficient specific activity of 370-450 GBq μmol-1, with a radiochemical purity of >99%, which will be suitable for human PET studies. The Royal Society of Chemistry 2011.