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Background  The synthesis of [ 11 C]L-deprenyl-D 2  for imaging of astrocytosis with positron emission tomography (PET) in neurodegenerative diseases has been previously reported. [ 11 C]L-deprenyl-D 2  radiosynthesis requires a precursor, L-nordeprenyl-D 2 , which has been previously synthesized from L-amphetamine as starting material with low overall yields. Here, we present an efficient synthesis of L-nordeprenyl-D 2  organic precursor as free base and automated radiosynthesis of [ 11 C]L-deprenyl-D 2  for PET imaging of astrocytosis. The L-nordeprenyl-D 2  precursor was synthesized from the easily commercial available and cheap reagent L-phenylalanine in five steps. Next,  N -alkylation of L-nordeprenyl-D 2  free base with [ 11 C]MeOTf was optimized using the automated commercial platform GE TRACERlab® FX C Pro.    Results  A simple and efficient synthesis of L-nordeprenyl-D 2  precursor of [ 11 C]L-deprenyl-D 2  as free base has been developed in five synthetic steps with an overall yield of 33%. The precursor as free base has been stable for 9 months stored at low temperature (−20 °C). The labelled product was obtained with 44 ± 13% ( n  = 12) (end of synthesis, decay corrected) radiochemical yield from [ 11 C]MeI after 35 min synthesis time. The radiochemical purity was over 99% in all cases and specific activity was (170 ± 116) GBq/μmol.    Conclusions  A high-yield synthesis of [ 11 C]L-deprenyl-D 2  has been achieved with high purity and specific activity. L-nordeprenyl-D 2  precursor as free amine was applicable for automated production in a commercial synthesis module for preclinical and clinical application.

An efficient preparation of labelling precursor of [11C]L-deprenyl-D2 and automated radiosynthesis