^18F-氟乙酸盐及其前体的合成和质量分析

Synthesis and quality analysis of sodium ^18F-fluoroacetate and its precursor

目的探讨^18F-氟乙酸盐（FAC）及其前体化合物2．甲磺酸基乙酸乙酯（EOMG）的合成和进行质量分析。方法改进前体化合物EOMG的合成方法，利用HPLC法测定该前体化合物的化学纯度，并通过各种光谱学手段对其结构进行鉴定。以EOMG为前体，用Explora GN模块合成^18F-FAC，再用Explora LC除去其中的化学杂质，HPLC法和放射性薄层色谱（TLC）法检测其放化纯、化学纯度和比活度。结果合成并鉴定了前体化合物EOMG，产率为70％，化学纯度为97．0％（按色谱峰面积计算）。合成了^18F-FAC，放化纯〉98％，且无明显的化学杂质，比活度为236．5MBq／μmol。结论该研究为制备有效、质量可控的^18F-FAC提供了依据。

Objective To synthesize and analyze sodium ^18F-fluoroacetate （FAC） and its precursor ethyl O-mesylglycolate （EOMG）. Methods EOMG was synthesized using modified method. Its chemi- cal purity was checked by HPLC and its structure was elucidated on the basis of spectral analyses. Final product of ^18F-FAC was synthesized based on general nucleophilic reactions module Explora GN using EOMG as a precursor. Liquid chromatography Explora LC was applied to get rid of its chemical impurities. Then HPLC and radio-thin layer chromatography were used to assay its radiochemical purity, chemical purity and specific activity. Results EOMG was synthesized and identified. Its yield was 70% and its chemical purity was 97.0% （calculated by chromatographic peak area）. The radiochemical purity of lSF-FAC was more than 98%, and its specific activity was 236.5 MBq/μmol. Conclusion This synthetic method for ^18F-FAC and its precursor can be defined as effective and hizhly auality-controlled.