Synthesis of 2??[18F] fluoro??3??[2 (S)??2??azetidinylmethoxy] pyridine, a highly potent radioligand for in vivo imaging central nicotinic acetylcholine receptors

…, M Bottlaender, F Hinnen, F Vaufrey…

Index: Dolle, Frederic; Valette, Heric; Bottlaender, Michel; Hinnen, Francoise; Vaufrey, Francoise; Guenther, Ilonka; Crouzel, Christian Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 5 p. 451 - 463

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Citation Number: 71

Abstract

Abstract This paper reports the synthesis of 2-fluoro-3-[2 (S)-2-azetidinylmethoxy] pyridine and its radiolabeling with fluorine-18 ([18 F] FK-K 222) by nucleophilic aromatic nitro-to- fluoro substitution in DMSO by conventional heating at 150 C for 20 min or by microwave activation at 100 Watt for 1 min. This fluoro compound is a closely related analog of the high affinity nicotinic ligand A-85380 (3-[2 (S)-2-azetidinylmethoxy] pyridine). This compound is ...