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Nicotinic acetylcholine receptors (nChRs) are involved in the various pharmacological effects or disease states. In order to study the central nChRs by PET or SPECT, some radioligands have been investigated. In this paper, the procedure for synthesis of 2-[18F]fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine (2-[18F]-A-85380), a potential PET ligand for in vivo imaging nicotinic acetylcholine receptor was described. 2-[18F]-A-85380 was prepared from the precursor, 2-nitro-3-[(1-(tert-butoxycarbonyl)-2-(S)-azetidinyl)methoxy]pyridine(4), which was synthesized with commercial (S)-2-azetid- inecarboxylic acid as starting material. The whole procedure for radiosynthesis and purification was executed in about 1h and 45-55% of the added fluorine-18 was found in the purified 2-[18F]-A-85380, with specific activity of 1.0-2.2×1011 Bq/μmol.
In order to study the central nChRs by PET or SPECT, some radioligands have been investigated. In this paper, the procedure for synthesis of 2- [18F] fluoro 3- [2 (S) -2-azetidinylmethoxy] pyridine (2- [18F] -A-85380), a potential PET ligand for in vivo imaging nicotinic acetylcholine receptor was described. 2- [18F] -A-85380 was was synthesized from the precursor 2-nitro-3 - [(1- (tert-butoxycarbonyl) -2- (S) -azzetidinyl) methoxy] pyridine acid as starting material. The whole procedure for radiosynthesis and purification was executed in about 1h and 45-55% of the added fluorine-18 was found in the purified 2- [18F] -A-85380, with a specific activity of 1.0-2.2 × 1011 Bq / μmol.