Two-step radiosynthesis of [18F]N-succinimidyl-4-fluorobenzoate ([18F]SFB)

被引：33

作者：

Glaser, Matthias ^{[1
]}

Arstad, Erik ^{[1
]}

Luthra, Sajinder K. ^{[1
]}

Robins, Edward G. ^{[1
]}

机构：

[1] Hammersmith Hosp, GE Healthcare, London W12 0NN, England

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2009年 / 52卷 / 7-8期

关键词：

N-succinimidyl; 4-fluorobenzoate; fluorine-18; fluorobenzaldehyde; PET; microwave; N-SUCCINIMIDYL 4-<F-18>FLUOROBENZOATE; POSITRON-EMISSION-TOMOGRAPHY; RGD PEPTIDE; LABELING PROTEINS; F-18; AGENT; CONJUGATION; RADIOPHARMACEUTICALS; NEUROTENSIN(8-13); EXPRESSION;

D O I：

10.1002/jlcr.1601

中图分类号：

Q5 [生物化学];

学科分类号：

070307 [化学生物学];

摘要：

The acylation reagent (F-18]N-succinimidyl-4-fluorobenzoate (F-18-SFB) has been prepared using a new two-step approach. The starting material p-[F-18]fluorobenzaldehyde (F-18-FBA) was obtained by an improved radiosynthesis with a decay-corrected radiochemical yield of 66 +/- 6 % (n=3). Reaction of F-18-FBA with (diacetoxyiodine)benzene and N-hydroxysuccinimide and preparative HPLC purification furnished 18F-SFB in an r.c.y. of 49 +/- 6 % (n=3), based on the starting radioactivity of F-18-FBA. The radiochemical purity of 18F-SFB was >99%. Alternatively, purification by solid phase extraction gave 18F-SFB with an r.c.y. of 77 +/- 9% (n=4) and a radiochemical purity of 89 +/- 5% (n=4). This radiochemical synthesis only used non-aqueous solvents, which simplifies the method and facilitates subsequent applications of F-18-SFB.

引用

页码：327 / 330

页数：4

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