Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2002, Vol. 13 ›› Issue (2): 92

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

LIU Ning, DING Yu-Shin1, WANG Tao1, GARZA V1, FOWLER J S2   

  1. Key Laboratory of Radiation Physics and Technology of Education Ministry of China. Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064;
    1 Chemistry Department, Brookhaven National Laboratory, Upton, NY11973, USA
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LIU Ning, DING Yu-Shin, WANG Tao, GARZA V, FOWLER J S. Synthesis of 2-[18F ]fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine as a radioligand for imaging nicotinic acetylcholine receptors.Nuclear Science and Techniques, 2002, 13(2): 92

Abstract: Nicotinic acetylcholine receptors (nhRs) 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), 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)-2azetid- inecarboxylic acid as starting material. The whole procedure for radiosynthesix 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 x 1011 Bq/μmol.

Key words: Nicotinic acetylcholine receptors, Precursor, Radioligand, 18F Radiosynthesis