Synthesis of 16α-[18F]fluoroestradiol-3,17β-disulphamate

被引:0
作者
Römer, J [1 ]
Füchtner, F [1 ]
Steinbach, J [1 ]
机构
[1] Forschungszentrum Rossendorf EV, Inst Bioorgan & Radiopharmaceut Chem, D-01314 Dresden, Germany
关键词
16 alpha-[F-18]fluoroestradiol-3,17 beta-disulphamate; F-18-labelled tracer; positron emission tomography; sulphamoylation; HPLC purification;
D O I
暂无
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis of 16 alpha-[F-18]fluoroestradiol-3,17 beta-disulphamate ([F-18]FESDS) is described. 16-alpha[F-18]Fluoroestradiol ([F-18]FES) is converted using excess sulphamoyl chloride in absolute acetonitrile in the presence of Kryptofix 2.2.2 and potassium carbonate using an automatically operating module. The required time for the synthesis related to end of bombardment is 3h, the maximum yield is 6%, and the maximum decay-corrected yield is 20%. The radiochemical purity of [F-18]FESDS is > 99%. The specific radioactivity of [F-18]FESDS is found to be between 150 and 200 GBq/mu mol.
引用
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页码:425 / 436
页数:12
相关论文
共 17 条
[11]  
Römer J, 1999, J PRAK CHEM-CHEM ZTG, V341, P574
[12]   Studies on the synthesis of 16 alpha-[F-18]fluoroestradiol [J].
Romer, J ;
Steinbach, J ;
Kasch, H .
APPLIED RADIATION AND ISOTOPES, 1996, 47 (04) :395-399
[13]   Automated production of 16α-[18F]fluoroestradiol for breast cancer imaging [J].
Römer, J ;
Füchtner, F ;
Steinbach, J ;
Johanssen, B .
NUCLEAR MEDICINE AND BIOLOGY, 1999, 26 (04) :473-479
[14]  
Schwarz Sigfrid, 1996, Drugs of the Future, V21, P49
[15]  
SPILLANE J, 1982, J CHEM SOC P1, P677
[16]  
STOCKLIN G, EUR J NUCL MED, V25, P1612
[17]   Improving the yield of 2-[F-18]fluoro-2-deoxyglucose using a microwave cavity [J].
Taylor, MD ;
Roberts, AD ;
Nickles, RJ .
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (05) :605-609