Efficient synthesis of the 18F-labelled 3-O-methyl-6-[18F]fluoro-L-DOPA

被引：19

作者：

Füchtner, F

Steinbach, J

机构：

[1] PET Zentrum Rossendorf, Forschungszentrum Rossendorf, Inst Bioorgan & Radiopharmaceut Chem, D-01314 Dresden, Germany

[2] Inst Interdisziplinare Isotopenforsch, D-04318 Leipzig, Germany

来源：

APPLIED RADIATION AND ISOTOPES | 2003年 / 58卷 / 05期

关键词：

3-O-methyl-6-[F-18]fluoro-L-DOPA; radiolabelled amino acid; electrophilic F-18-fluorination; PET-radiotracer;

D O I：

10.1016/S0969-8043(03)00062-9

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The F-18-labelled amino acid derivative 3-O-methyl-6-[F-18]fluoro-L-DOPA ([F-18]OMFD) is a potential radiotracer for imaging tumour tissue using positron emission tomography. The precursor N-formyl-3-O-methyl-4-O-boc-6-trimethylstannyl-L-DOPA-ethyl ester enables direct electrophilic radiofluorination by stereoselective destannylation. After partial hydrolysis, optimized HPLC purification and sterile filtration, the [F-18]OMFD obtained with high radiochemical purity and ready for use. The total synthesis time is about 50min and the radiochemical yield achieved is 20-25% (decay corrected, related to [F-18]F-2)- It was demonstrated that [F-18]OMFD could be produced routinely and reliably for clinical use. [F-18]FDOPA-preparation devices can be used with minor modifications. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：575 / 578

页数：4

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