采用离子液体作为相转移催化剂一步法合成^(18)F-FLT的方法研究

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

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0.1ml1MK2CO3,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。

Objective： The synthesis ^18F-FLT with one pot method used 1-Butyl-3-methylimidazolium trifluoromethanesul- fonate（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.