Automated synthesis of hypoxia imaging agent [18F]FMISO based upon a modified Explora FDG4 module

被引:14
作者
Wang, Mingwei [1 ]
Zhang, Yingjian [1 ]
Zhang, Yongping [1 ]
Yuan, Huiyu [1 ]
机构
[1] Fudan Univ, PET Ctr, Dept Nucl Med, Dept Oncol,Shanghai Med Coll, Shanghai 200032, Peoples R China
基金
中国国家自然科学基金;
关键词
NECK-CANCER; FLUOROMISONIDAZOLE; HEAD; PET;
D O I
10.1007/s10967-008-7395-8
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
A new automated synthesis procedure of 1-H-1-(3-[F-18]fluoro-2-hydroxypropyl)-2-nitroimidazole ([F-18]FMISO), a specific hypoxia imaging agent with great significances for the noninvasive, dynamic hypoxia evaluation of cancer, was developed by modifying Explora FDG(4) module, a commercial [F-18]FDG production system, in this study. Its radiochemical synthesis was carried out via two sequent reaction steps, i.e. the nucleophilic displacement of labeling precursor 1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydropyranyl-3-O-tosyl-propanediol (NITTP) with activated F-18- ion at 100 A degrees C for 8 minutes, and the following hydrolysis with 1M HCl at 100 A degrees C for 5 minutes and neutralization with 1M NaOH. Two-pot reaction with two independent separations was adopted to assure the good separation of final product via solid phase extraction (SPE) based upon combined Sep-pak cartridges instead of high performance liquid chromatography (HPLC). This fast, reliable preparation route of F-18-FMISO could complete within 50 minutes with about 55% of high radiochemical yield (with decay correction) and more than 98% of good radiochemical purity. The modified module could perform multiple runs of production of [F-18]FMISO.
引用
收藏
页码:149 / 155
页数:7
相关论文
共 12 条
[1]   A robotic synthesis of [18F]fluoromisonidazole ([18F]FMISO) [J].
Chang, C. W. ;
Chou, T. K. ;
Liu, R. S. ;
Wang, S. J. ;
Lin, W. J. ;
Chen, C. H. ;
Wang, H. E. .
APPLIED RADIATION AND ISOTOPES, 2007, 65 (06) :682-686
[2]  
Cher LM, 2006, J NUCL MED, V47, P410
[3]  
Eschmann SM, 2005, J NUCL MED, V46, P253
[4]  
Graham MM, 1997, J NUCL MED, V38, P1631
[5]  
Hung JC, 2002, J NUCL MED, V43, P1495
[6]   Preparation of fluorine-18-labelled fluoromisonidazole using two different synthesis methods [J].
Kämäräinen, EL ;
Kyllönen, T ;
Nihtilä, O ;
Björk, H ;
Solin, O .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2004, 47 (01) :37-45
[7]   AN EFFICIENT RADIOSYNTHESIS OF [F-18] FLUOROMISONIDAZOLE [J].
LIM, JL ;
BERRIDGE, MS .
APPLIED RADIATION AND ISOTOPES, 1993, 44 (08) :1085-1091
[8]   Fully automated synthesis of [18F]fluoromisonidazole using a conventional [18F]FDG module [J].
Oh, SJ ;
Chi, DY ;
Mosdzianowski, C ;
Kim, JY ;
Gil, HS ;
Kang, SH ;
Ryu, JS ;
Moon, DH .
NUCLEAR MEDICINE AND BIOLOGY, 2005, 32 (08) :899-905
[9]   Preparation of [18F]fluoromisonidazole by nucleophilic substitution on THP-protected precursor:: Yield dependence on reaction parameters [J].
Patt, M ;
Kuntzsch, M ;
Machulla, HJ .
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 1999, 240 (03) :925-927
[10]  
[唐刚华 Tang Ganghua], 2005, [核化学与放射化学, Journal of Nuclear and Radiochemistry], V27, P43