192191-50-7Relevant articles and documents
Automated radiosynthesis of no-carrier-added [S-fluoromethyl-18F] fluticasone propionate as a radiotracer for lung deposition studies with PET
Aigbirhio, Franklin I.,Carr, Richard M.,Pike, Victor W.,Steel, Colin J.,Sutherland, Derek R.
, p. 567 - 584 (1997)
Fluticasone propionate [(S)-fluoromethyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α -(propionyloxy)-androsta-1,4-diene-17β-carbothioate; FP] is a potent anti-inflammatory steroid with several therapeutic indications, including use as an anti-asthmatic drug when administered as sized particles by inhalation from a pressurised metered-dose inhaler (pMDI). FP was successfully labelled with fluorine-18 (t( 1/4 ) = 109.6 min: β+ = 100%) by displacement of tosylate with cyclotron-produced no-carrier-added [18F]fluoride in an (S)-tosylmethyl precursor prepared from the known (S)-chloromethyl analogue of FP. Radiochemically pure [S-/fluoromethyl-18]FP was separated by reverse phase HPLC in 35% radiochemical yield (decay-corrected) within 80 min from the end of radionuclide production (as verified by, radio-HPLC, LC-MS and LC-NMR). The radiosynthesis was automated for the safe production of high radioactivities (20-50 mCi) of [18F]FP in a lead-shielded hot-cell for subsequent incorporation into formulated FP particles within a pMDI and subsequent study of FP deposition in human lung using positron emission tomography (PET).
