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细胞凋亡显像剂18 F-M L-10前体合成及放射性标记

桂媛 徐志宏 张晓军 李云刚 刘健 张锦明

核化学与放射化学2016,Vol.38Issue(3):188-192,5.
核化学与放射化学2016,Vol.38Issue(3):188-192,5.DOI:10.7538/hhx.2016.38.03.0188

细胞凋亡显像剂18 F-M L-10前体合成及放射性标记

Synthesis Precursor of Apoptosis Imaging Agent 18 F-ML-10 and Its Radiolabing With 18 F

桂媛 1徐志宏 1张晓军 2李云刚 2刘健 2张锦明2

作者信息

  • 1. 华益科技有限公司,江苏 常熟 215522
  • 2. 中国人民解放军总医院 核医学科,北京 100853
  • 折叠

摘要

Abstract

18 F‐2‐(5‐fluoro‐pentyl)‐2‐methyl malonic acid(18 F‐M L‐10) is one of the competitive candidate for apoptosis imaging with PET .ML‐10 as reference and its OTs derivative (dieth‐yl 2‐methyl‐2‐(5‐(tosyloxy)pentyl) malonate) as precursor for labeling with fluorine‐18 were prepared .18 F‐ML‐10 was synthesized via nucleophilic substitution and base hydrolysis .The 18 F‐ML‐10 injection was got by semi‐HPLC and solid‐extraction‐preparation via home MF‐2V‐IT‐1 module .The synthesis yield of 18 F‐ML‐10 is (25.3 ± 4.7)% (n= 16 ,no corrected decay ) ,and the specific activity is 740 PBq/mol .T he radiochemical purity is over 99% .T he residuary acetonitrile in the injection is (0.015 ± 0.01)% (w) .The K2.2.2 mass concentra‐tion in the injection is low than 10 mg/L .The injection is free of bacteria and pyrogen .It can be used for clinical research .

关键词

18 F/放射性合成/放射药物/细胞凋亡/PET

Key words

18 F/radiosynthesis/radiopharmaceuticals/apoptosis/PET

分类

医药卫生

引用本文复制引用

桂媛,徐志宏,张晓军,李云刚,刘健,张锦明..细胞凋亡显像剂18 F-M L-10前体合成及放射性标记[J].核化学与放射化学,2016,38(3):188-192,5.

基金项目

国家自然科学基金资助项目 ()

核化学与放射化学

OA北大核心CSCDCSTPCD

0253-9950

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