Automatic Synthesis of N-Succinimidyl-4-18FFluorobenzoate
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Graphical Abstract
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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 trifluoromethanesulfonate 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 CH3CN 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 decaycorrected 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.
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