p‐[18F]‐MPPF: A potential radioligand for PET studies of 5‐HT1A receptors in humans

The purpose of this study was to develop a radiopharmaceutical that could be used to selectively image 5‐HT1A receptors with positron emission tomography (PET) No‐carrier‐added 4‐(2′‐methoxyphenyl)‐1‐[2′‐(N‐2′‐pyridinyl)‐p‐[18F]fluorobenzamido]ethylpiperazine (p‐[18F]‐MPPF, 2) was synthesized by the nucleophilic substitution of the corresponding nitro precursor 1 with K[18F]/Kryptofix 2.2.2. in dimethyl sulfoxide (DMSO) at 140°C for 20 min followed by purification with high‐performance liquid chromatography (HPLC) in 10% yield in a synthesis time of 90 min from end of bombardment (EOB). Specific activity was 1–4 Ci/μM.