| Popis: |
A detailed and improved synthetic procedure to produce NCA 6-[ 18 F]fluoro- l -dopa (6-FDOPA) is described. A remotely-operable system for its routine production was built and tested for stable and reproducible tracer production ( n > 20). Commercially available 6-nitroveratraldehyde or 6-nitropiperonal served as precursor for [ 18 F]fluoride displacement reaction. The resulting 6-[ 18 F]fluoroaldehyde was condensed with 2-phenyl-5-oxazolone, followed by reductive hydrolysis, to obtain, after HPLC purification, a racemic mixture of 6-FDOPA. The optical isomers were resolved on a preparative reverse phase chiral column to obtain pure 6-FDOPA. The chemical, radiochemical and enantiomeric purity was established and was reproducible. PET Scans in monkeys were carried out to establish viability of NCA 6-DOPA as a PET tracer. This represents first examples of use of NCA 6-FDOPA in assessing dopaminergic functions of brain. |
