Setoperone Explained

Setoperone is a compound that is a ligand to the 5-HT_2A receptor.It can be radiolabeled with the radioisotope fluorine-18 and used as a radioligand with positron emission tomography (PET).Several research studies have used the radiolabeled setoperone in neuroimaging for the studying neuropsychiatric disorders, such as depression^[1] or schizophrenia.^[2]

Synthesis

The starting material is called 6-(2-hydroxyethyl)-7-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-5-one, CID:15586462 (1). Halogenation of this with hydrobromic acid in acetic acid gives CID:15586463 (2). Sn2 alkylation with 4-(4-fluorobenzoyl)piperidine [56346-57-7] (3) under Finkelstein reaction conditions affords setoperone (4).

See also

• Altanserin
• Ketanserin
• Pirenperone
• Ritanserin

Notes and References

1. Jeffrey H. Meyer, Shitij Kapur, Sylvain Houle, Jean DaSilva, Beata Owczarek, Gregory M. Brown, Alan A. Wilson and Sidney H. Kennedy. Prefrontal Cortex 5-HT2 Receptors in Depression: An [¹⁸F]Setoperone PET Imaging Study. American Journal of Psychiatry. 156. 1029–1034. 10401447. 7. July 1, 1999 . 10.1176/ajp.156.7.1029. 453720.
2. Ralph Lewis, Shitij Kapur, Corey Jones, Jean DaSilva, Gregory M. Brown, Alan A. Wilson, Sylvain Houle and Robert B. Zipursky. Serotonin 5-HT₂ Receptors in Schizophrenia: A PET Study Using [¹⁸F]Setoperone in Neuroleptic-Naive Patients and Normal Subjects. American Journal of Psychiatry. 156. 72–78. 9892300. 1. January 1, 1999 . 10.1176/ajp.156.1.72.