自动化合成N-琥珀酰亚胺-4-[^(18)F]氟苯甲酸酯  

Automatic Synthesis of N-Succinimidyl-4-[^(18)F] Fluorobenzoate

作　　者：刘晓飞[1] 张锦明[1] 田嘉禾[1] 陈英茂[1] 

机构地区：[1]解放军总医院核医学科,北京100853

出　　处：《核化学与放射化学》2008年第1期29-33,共5页Journal of Nuclear and Radiochemistry

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([18F]SFB)。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([18F]FBA),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[18F]SFB,Sep-Pak C18固相柱分离得纯[18F]SFB。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[18F]SFB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。N-succinimidyl-4-[^18 F]fluorobenzoate（[^18 F] SFB） 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 （[^18 F]FBA）. After purifying through Sep-Pak C18 cartridge, [^18 F]FBA was dissolved with TSTU in CH3CN and reacted to produce [^18 F]SFB. 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 [^18F]SFB were much higher. The radiochemical yield of [^18F]SFB is （28.2± 1.9） （n=5）, and radiochemical purity of [^18F]SFB is more than 90%. The whole reaction time is only 45 min from ^18F-F- to [^18F]SFB. 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.

关 键 词：[^18F]SFB 自动化 多功能化学合成模块 

分 类 号：O628.51[理学—有机化学]