自动化合成N-琥珀酰亚胺-4-18F氟苯甲酸酯

    Automatic Synthesis of N-Succinimidyl-4-18FFluorobenzoate

    • 摘要: 通过自动化多功能化学合成模块,在线合成N-琥珀酰亚胺-4-18F氟苯甲酸酯(18FSFB)。标记前体4-三甲基胺苯甲酸乙酯三氟甲基磺酸盐与干燥的18F-发生亲核反应,生成4-18F氟苯甲酸乙酯,碱水解得到4-18F-氟苯甲酸(18FFBA),经Sep-Pak C18固相柱分离,加O-(N-琥珀酰亚胺)N,N,N′,N′-四甲基脲四氟硼酸盐(TSTU)乙腈溶液反应,生成18FSFB, Sep-Pak C18固相柱分离得纯18FSFB。 在115 ℃,密封条件间隔通氮气加热10 min亲核反应,用NaOH水解保护基团,得到18FSFB的不校正合成效率为(28.2±1.9)% (n=5),放射化学纯度大于90%,总的合成时间为45 min。

       

      Abstract: N-succinimidyl-4-18Ffluorobenzoate(18FSFB) was prepared using a multifunction chemistry process control unit module. The dried K222/18F- was resolubilized with a solution of 4-trimethlammoniumbenzoate trifluoromethanesulfonate and reacted to produce ethyl-4-18F fluorobenzoate. The ethylester was subsequently hydrolyzed using alkali to obtain the 4-18F fluorobenzoic acid(18FFBA). After purifying through Sep-Pak C18 cartridge, 18FFBA was dissolved with TSTU in CH3CN and reacted to produce 18FSFB. The nucleophilic reaction reated for 10 min at 115 ℃ in the covered vial, mixturing solvents with netrogen for several seconds and the ethylester was subsequently hydrolyzed using alkali. The decaycorrected yields of 18FSFB were much higher. The radiochemical yield of 18FSFB is (28.2±1.9)% (n=5), and radiochemical purity of 18FSFB is more than 90%. The whole reaction time is only 45 min from 18F-F- to 18FSFB. The whole reaction time can be shorten and the yield of product is high by using the multifunction chemistry process control unit module. It is a quick and highly efficient method for labeling bioactive compound.

       

    /

    返回文章
    返回