Synthesis and labeling of 5'-O-(4,4'-dimethoxytrityl)-2,3'-anhydr othymidine for [18F]FLT preparation

被引：0
|
作者：
A. Blocher
M. Kuntzsch
R. Wei
H.-J. Machulla
机构：
[1] PET-Zentrum,Sektion Radiopharmazie
[2] Universitätsklinikum Tübingen,undefined
来源：
Journal of Radioanalytical and Nuclear Chemistry | 2002年 / 251卷
关键词：
Physical Chemistry; Hydrolysis; DMSO; Inorganic Chemistry; Deoxythymidine;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
For in vivo measurement of DNA synthesis in the patient"s tumour 3"-[18F]fluoro-3"-deoxythymidine (FLT) has been shown to be very promising. As a new labeling precursor 5"-O-(4,4"-dimethoxytrityl)-2,3"-anhydrothymidine (DMTThy) was chosen and an organic synthesis was developed including NMR and MS data for characterisation. The 18F-labeling of DMTThy can be performed within 30 minutes in radiochemical yields of almost 20% when using polar solvents such as DMF or DMSO and a temperature of 160 °C. Hydrolysis is completed with 1N HCl at 50 °C within 10 minutes without losses.
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页码：55 / 58
页数：3
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