Synthesis of 2-[18F]fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine as a radioligand for imaging nicotinic acetylcholine receptors

Synthesis of 2-[¹⁸F]fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine as a radioligand for imaging nicotinic acetylcholine receptors

LIU Ning，

DING Yu-Shin，

WANG Tao，

GARZA V，

FOWLER J S

Nuclear Science and Techniques

Vol.13, No.2

pp.92-97

Published in print 01 May 2002

CLC：O615, R817.4

20000

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.

Nicotinic acetylcholine receptorsPrecursorRadioligand18F. Radiosynthesis

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