采用离子液体作为相转移催化剂一步法合成18F-FLT的方法研究

辛军; 李宏利; 郭启勇; 赵周社

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中国临床医学影像杂志 ›› 2007, Vol. 18 ›› Issue (5) : 348-350.

论著

采用离子液体作为相转移催化剂一步法合成18F-FLT的方法研究

辛军1，李宏利2，郭启勇1，赵周社2

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Synthetic methods research of 18F-FLT as phase transfer calalyst by ionic liquid with one pot methodology

XIN Jun1, LI Hong-li2, GUO Qi-yong1, ZHAO Zhou-she2

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摘要

目的：采用1-丁基-3-甲基咪唑三氟甲基磺酸酯（BMI）离子液体作为相转移催化剂（PTC）一步法合成18F-FLT。为临床提供简单、快速、稳定的18F-FLT合成方法。材料和方法：从加速器获得18F离子分离后，以BMI离子液体作为相转移催化剂、{3-N-叔丁基酰基-[5’-O-（4，4’-二甲氧三苯甲基）－2’-脱氧－3’－O－（4-硝基苯磺酰）－b－D－5呋喃]}胸腺嘧啶作为前体对在不同K2CO3体积、不同加热温度下及前体量时对最佳合成效率进行研究。结果：采用0.1ml 1M K2CO3，在130℃加热温度、前体30mg获得最高的合成效率。结论：采用离子液体作为PTC能够快速、稳定合成18F-FLT。

Abstract

Objective: The synthesis 18F-FLT with one pot method used 1-Butyl-3-methylimidazolium trifluoromethanesulfonate(BMI) ionic liquid(IL) as phase transfer catalysis(PTC). To develop the simple, quickly, stability synthesis 18F-FLT method for clinical application. Materials and Methods: To separate 18F ionic transferred from cyclotron first. We study 18F-FLT productivity with the different K2CO3 volume, heat temperature and precursor quantity used 3-N-tert-Butoxycarbonyl-[5’-O-(4, 4’-dimethoxytripphenylmethyl)-2’-deoxy-3’-O-(4-nitrobenzenesulfonyl)-b-D-threopentofuranosyl] thymine as precursor and BMI as PTC. Results: We can get the highest yield of 18F-FLT synthesis with 0.1ml 1M, 130℃ and 30mg precursor. Conclusions: BMI IL can be used PTC to synthesize 18F-FLT which has fast higher yield and high stability.

导出引用

辛军;李宏利;郭启勇;赵周社. 采用离子液体作为相转移催化剂一步法合成18F-FLT的方法研究[J]. 中国临床医学影像杂志. 2007, 18(5): 348-350

XIN Jun;LI Hong-li;GUO Qi-yong;ZHAO Zhou-she. Synthetic methods research of 18F-FLT as phase transfer calalyst by ionic liquid with one pot methodology[J]. Journal of China Clinic Medical Imaging. 2007, 18(5): 348-350

中图分类号： Ｒ817.4 Ｒ817.9