1 Center for Nuclear Technologies, Technical University of Denmark2 The Hevesy Laboratory, Center for Nuclear Technologies, Technical University of Denmark
The first example of transition metal mediated enantioselective radiofluorination of epoxides is reported. The procedure utilizes gaseous [18F]HF in a combination with (−)tetramisole and (R,R)-Co(salen), giving the corresponding (S,S)-18F-fluorohydrines in 78–93% radiochemical yield (RCY) and 20–46% enantioselectivities (ee). The use of this methodology allowed for a single step radiosynthesis of [18F]F-MISO, which took 1.5h and after solid phase-based purification delivered [18F]F-MISO in 81%/45% analytical/preparative RCY and 55% ee.
Journal of Fluorine Chemistry, 2013, Vol 156, p. 130-135
Radiofluorination; Metal mediated; F-MISO; PET; [18F]