摘要
乏氧是大部分实体瘤的一个固有特点,对放疗和化疗均产生很大的阻抗效应,严重影响肿瘤的治疗效果,往往导致不良预后。1-H-1-(3-[18F]氟-2-羟基丙基)-2-硝基咪唑(18F-FMISO)是一种特异性乏氧显像剂,临床上可通过PET/CT检查,评价肿瘤乏氧状况,指导放化疗治疗计划。本文基于对ExploraFDG4合成模块的合理改装发展了18F-FMISO的一种新的自动化合成方法,以1-(2’-硝基-1’-咪唑基)-2-氧-四氢吡喃基-3-氧-甲苯磺酰基-丙二醇为标记前体化合物,采用"两锅法"反应和硅胶柱分离,实现了18F-FMISO快速、可靠的自动化合成,合成时间约为50min,放射化学产率为55%左右(衰变校正之后),放射化学纯度大于98%。
Hypoxia is a major inherent characteristic for the most of solid tumors and produces severe treatment resistance to radiotherapy and chemotherapy of tumors and often results in poor prognosis. 1-H-1-（3-[^18F]fluoro-2-hydroxypropyl）-2- nitroimidazole（lSF-FMISO）is a specifc hypoxia imaging agent and has been applied into clinic to evaluate tumor hypoxia status and guide treatment plan of radiotherapy and chemotherapy by PET/CT. A new automated synthesis procedure of lSF-FMISO was developed by modifying the Explora FDG4 module and taking 1-（2＇-nitro-l＇-imidazolyl）-2-O-tetrahydropyranyl- 3-O-tosyl-propanediol as labeling precursor in this study. Two-pot reaction was adopted to assure good separation of the final product via solid phase extraction based upon combined Sep-pak cartridges instead of HPLC. This fast reliable preparation route of ^18F-FMISO could be completed in about 50 rain with about 55% of radiochemical yield and over 98% of radiochemical purity.
出处
《核技术》
EI
CAS
CSCD
北大核心
2008年第6期460-464,共5页
Nuclear Techniques
基金
上海市卫生局青年科研项目(2006Y11)
