Facile synthesis of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) for protein labeling

被引：74

作者：

Tang, G. ^{[1
]}

Zeng, Wenbin ^{[2
]}

Yu, Meixiang ^{[2
]}

Kabalka, G. ^{[1
]}

机构：

[1] Univ Tennessee, Grad Sch Med, Dept Chem & Radiol, Knoxville, TN 37920 USA

[2] Univ Tennessee, Grad Sch Med, Dept Med, Knoxville, TN 37920 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2008年 / 51卷 / 1-2期

关键词：

protein labeling; F-18; VEGF; SFB; Avastin; one-pot; radiosynthesis;

D O I：

10.1002/jlcr.1481

中图分类号：

Q5 [生物化学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

An efficient preparation of N-succinimidyl 4-[F-18]fluorobenzoate ([F-18]SFB) based on a convenient three-step, one-pot procedure is described. [18F] Fluorination of the precursor ethyl 4-(trimethylammonium triflate)benzoate gave ethyl 4-[F-18]fluorobenzoate. Saponification of the ethyl 4-[F-18]fluorobenzoate with aqueous tetrapropylammoniurn hydroxide yielded the corresponding 4-[F-18]fluorobenzoate salt ([F-18]FBA), which was then treated with NNN,N'-tetramethyl-O-(N-succinimidyl)uronium hexafluorophosphate. The purified [F-18]SFB was used for the labeling of Avastin (TM) (Bevacizumab) through [F-18]fluorobenzoylation of the Avastin's alpha-amino groups. The decay-corrected radiochemical yields of [F-18]SFB were as high as 44% (based on [F-18]fluoride (n = 10) with a synthesis time of less than 60 min. [F-18]Avastin was produced in decay-corrected radiochemical yields of up to 42% (n = 5) within 30 min (based on [F-18]SFB). The radiochemical purities of [F-18]SFB and [F-18]Avastin were greater than 95%.

引用

页码：68 / 71

页数：4

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