一种由甲磺酸盐前体一步自动合成高放射化学产率的¹⁸F-FECNT的方法。
A one-step automated high-radiochemical-yield synthesis of 18F-FECNT from mesylate precursor.
作者信息
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
机构信息
School of Medicine and Pharmaceutics, Jiangnan University, Wuxi, PR China.
出版信息
Appl Radiat Isot. 2008 Dec;66(12):1881-5. doi: 10.1016/j.apradiso.2008.05.002. Epub 2008 May 15.
2Beta-carbomethoxy-3beta-(4-chlorophenyl)-8-(2-[(18)F]fluoroethyl)nortropane ((18)F-FECNT) is a potential dopamine transporter imaging agent. In this article, a new mesylate precursor was prepared and a one-step automated synthesis of (18)F-FECNT was developed. The mesylate precursor (4) was synthesized from 2beta-carbomethoxy-3beta-(4-chlorophenyl)tropane (1) by N-demethylation, hydroxyethylation followed by mesylation at a total yield of 47%. [(18)F]fluorination was performed by heating 4mg mesylate precursor and K[(18)F] in 1 ml acetonitrile at 90 degrees C for 20 min. The crude (18)F-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 radiochemical purity of 98.4% and a decay corrected radiochemical yield of 33+/-9% (and the uncorrected radiochemical yield was 19+/-5%, n=5). The duration of the total procedure was 80-90 min.
2β-甲氧羰基-3β-(4-氯苯基)-8-(2-[(¹⁸)F]氟乙基)去甲托烷((¹⁸)F-FECNT)是一种潜在的多巴胺转运体显像剂。本文制备了一种新的甲磺酸盐前体，并开发了(¹⁸)F-FECNT的一步自动化合成方法。甲磺酸盐前体(4)由2β-甲氧羰基-3β-(4-氯苯基)托烷(1)经N-去甲基化、羟乙基化，然后甲磺酰化反应合成，总收率为47%。通过将4mg甲磺酸盐前体与K[(¹⁸)F]在1ml乙腈中于90℃加热20分钟进行[(¹⁸)F]氟化反应。粗品(¹⁸)F-FECNT的放射性标记产率为48%。经制备型高效液相色谱(HPLC)纯化后，得到最终的(¹⁸)F-FECNT产品，其放射化学纯度为98.4%，衰变校正后的放射化学产率为3³±9%（未校正的放射化学产率为19±5%，n = 5）。整个过程持续时间为80 - 90分钟。
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