A one-step automated high-radiochemical-yield synthesis of F-18-FECNT from mesylate precursor

作者：Chen Zheng Ping; Wang Song Pei; Li Xiao Min; Liu Chun Yi; Tang Jie; Cao Guo Xian; Luo Shi Neng; Zhang Lian Fen; Jin Jian^*

来源：Applied Radiation and Isotopes, 2008, 66(12): 1881-1885.

DOI：10.1016/j.apradiso.2008.05.002

• F-18-FECNT
• Automated synthesis
• One-step
• Dopamine transporter
• PET

2 beta-Carbomethoxy-3 beta-(4-chlorophenyl)-8-(2-[F-18]fluoroethyl)nortropane (F-18-FECNT) is a potential dopamine transporter imaging agent. In this article, a new mesylate precursor was prepared and a one-step automated synthesis of 18F-FECNT was developed. The mesylate precursor (4) was synthesized from 2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropane (1) by N-demethylation, hydroxyethylation followed by mesylation at a total yield of 47%. [ F-18]fluorination was performed by heating 4 ring mesylate precursor and K[F-18] in 1 ml acetonitrile at (90)degrees C for 20 min. The crude F-18-FECNT was obtained with a radiolabeling yield of 48%. After purification by preparative high performance liquid chromatography (HPLC), the final 18 F-FECNT product was obtained with a radiochernical purity of 98.4% and a decay corrected radiochemical yield of 33 +/- 9% (and the uncorrected radiochernical yield was 19 +/- 5%, n = 5). The duration of the total procedure was 80-90 min.

• 出版日期2008-12
• 单位江南大学; 江苏省原子医学研究所