Setoperone
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Setoperone (INN; USAN; developmental code name R-52245) is a compound that is a ligand to the 5-HT2A receptor.[1] 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[2] or schizophrenia.[3] The drug was first described by at least 1984.[1]
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| Other names | R-52245; R52245 |
| Drug class | Serotonin 5-HT2A receptor antagonist |
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| Formula | C21H24FN3O2S |
| Molar mass | 401.50 g·mol−1 |
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Chemistry
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).