Journal of labelled compounds and radiopharmaceuticals p. 567 - 584 (1997)
Update date:2022-08-04
Topics:
Aigbirhio, Franklin I.
Carr, Richard M.
Pike, Victor W.
Steel, Colin J.
Sutherland, Derek R.
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).
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Doi:10.1002/jhet.5570340331
(1997)Doi:10.1016/S0040-4020(97)90397-5
(1997)Doi:10.1039/jr9390000610
(1939)Doi:10.1055/s-1997-1405
(1997)Doi:10.1021/jm970020k
(1997)Doi:10.1039/a703008h
(1997)