Synthesis and stability of S-(2-[18F]fluoroethyl)-L-homocysteine for potential tumour imaging

被引:10
作者
Bourdier, Thomas [1 ]
Fookes, Christopher J. R. [1 ]
Pham, Tien Q. [1 ]
Greguric, Ivan [1 ]
Katsifis, Andrew [1 ]
机构
[1] Australian Nucl Sci & Technol Org, Radiopharmaceut Res Inst, Menai, NSW 2234, Australia
关键词
S-(2-[F-18]fluoroethyl)-L-homocysteine; FEHCys; amino acids; nucleophilic [F-18]-fluorination;
D O I
10.1002/jlcr.1539
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The F-18 labelled methionine derivative S-(2-[F-18]fluoroethyl)-L-homocysteine ([F-18]FEHCys) was prepared by a one-pot two-step synthesis via the protected S-(2-bromoethyl)-L-homocysteine 1 and S-(2-chloroethyl)-L-homocysteine 2 precursors. The bromoethyl derivative 1 gave higher radiochemical yields (40% at 5 min) at 100 degrees C compared with the chloro-analogue (22% at 100 C in 30 min). However, [F-18]FEHCys was found to be unstable in aqueous systems being transformed to the corresponding hydroxyl derivative within 20 min.
引用
收藏
页码:369 / 373
页数:5
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