Efficient synthesis and formulation of (R)‐(−)‐[11C]Deprenyl,a selective radioligand for the quantification of MAO‐B activity using PET

Carbon‐11 labeled (R)‐(?)‐Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)‐B activity with PET. In this paper, its radiosynthesis is re‐investigated and oriented towards the preparation of multi‐milliCuries of radiotracer. Typically, using no‐carrier‐added [¹¹C]methyl triflate as the alkylating agent, 140–190 mCi (5.1–7.0 GBq) of (R)‐(?)‐[¹¹C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/μmol (29.6–44.4 GBq/μmol). The high efficiency of these radiosyntheses allows for multi‐injection protocols and kinetic approaches for absolute quantification of the tracer. Copyright © 2002 John Wiley & Sons, Ltd.