自动化合成N-琥珀酰亚胺-4-[18F]氟苯甲酸酯

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。

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

N-succinimidyl-4-¹⁸F]fluorobenzoate（¹⁸F]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（¹⁸F]FBA）. After purifying through Sep-Pak C18 cartridge, ¹⁸F]FBA was dissolved with TSTU in CH3CN and reacted to produce ¹⁸F]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.