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首页> 外文期刊>Journal of Labelled Compounds and Radiopharmaceuticals >A facile automated synthesis of N-succinimidyl 4-[ 18F] fluorobenzoate ([ 18F]SFB) for 18F-labeled cell-penetrating peptide as PET tracer
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A facile automated synthesis of N-succinimidyl 4-[ 18F] fluorobenzoate ([ 18F]SFB) for 18F-labeled cell-penetrating peptide as PET tracer

机译：以18F标记的细胞穿透肽作为PET示踪剂的N-琥珀酰亚胺基4- [18F]氟苯甲酸酯（[18F] SFB）的自动合成

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A fully automated synthesis of N-succinimidyl 4-[ 18F] fluorobenzoate ([ 18F]SFB) was carried out by a convenient three-step, one-pot procedure on the modified TRACERlab FX FN synthesizer, including [ 18F]fluorination of ethyl 4-(trimethylammonium triflate)benzoate as the precursor, saponification of the ethyl 4-[ 18F]fluorobenzoate with aqueous tetrapropylammonium hydroxide instead of sodium hydroxide, and conversion of 4-[ 18F]fluorobenzoate salt ([ 18F]FBA) to [ 18F]SFB treated with N,N,N′,N′- tetramethyl-O-(N-succinimidyl)uranium tetrafluoroborate (TSTU). The purified [ 18F]SFB was used for the labeling of Tat membrane-penetrating peptide (containing the Arg-Lys-Lys-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Pro-Leu-Gly- Leu-Ala-Gly-Glu-Glu-Glu-Glu-Glu-Glu-Glu sequence, [ 18F]CPP) through radiofluorination of lysine amino groups. The uncorrected radiochemical yields of [ 18F]SFB were as high as 25-35% (based on [ 18F] fluoride) (n = 10) with a synthesis time of ～40 min. [ 18F]CPP was produced in an uncorrected radiochemical yields of 10-20% (n = 5) within 30 min (based on [ 18F]SFB). The radiochemical purities of [ 18F]SFB and [ 18F]CPP were greater than 95%.
机译：N-琥珀酰亚胺基4- [18F]氟苯甲酸酯（[18F] SFB）的全自动合成通过便利的三步一锅法在改良的TRACERlab FX FN合成器上进行，包括乙基4的[18F]氟化。 -（三氟甲磺酸三甲基铵）苯甲酸酯为前体，用氢氧化四丙基铵代替氢氧化钠将4- [18F]氟苯甲酸乙酯皂化，并将4- [18F]氟苯甲酸盐（[18F] FBA）转化为[18F] SFB用N，N，N'，N'-四甲基-O-（N-琥珀酰亚胺基）四氟硼酸铀（TSTU）处理。纯化的[18F] SFB用于标记Tat膜穿透肽（包含Arg-Lys-Lys-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Pro-Leu-Gly-Leu- Ala-Gly-Glu-Glu-Glu-Glu-Glu-Glu-Glu序列，[18F] CPP）通过赖氨酸氨基的放射性氟化。 [18 F] SFB的未经校正的放射化学产率高达25-35％（基于[18 F]氟化物）（n = 10），合成时间约为40分钟。 [18F] CPP在30分钟内以10-20％（n = 5）的未校正放射化学产率产生（基于[18F] SFB）。 [18F] SFB和[18F] CPP的放射化学纯度大于95％。

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