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

被引：17

作者：

Blocher, A ^{[1
]}

Kuntzsch, M ^{[1
]}

Wei, R ^{[1
]}

Machulla, HJ ^{[1
]}

机构：

[1] Univ Klinikum Tubingen, PET Zentrum, Sekt Radiopharm, D-72076 Tubingen, Germany

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2002年 / 251卷 / 01期

关键词：

D O I：

10.1023/A:1015042227131

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

For in vivo measurement of DNA synthesis in the patient's tumour 3'-[F-18]fluoro-3'-deoxythymidine (FLT) has been shown to be very promising. As a new labeling precursor 5'-O-(4,4'-dimethoxytrityl)-2,3'-anhydrothymidine (DNITThy) was chosen and an organic synthesis was developed including NMR and MS data for characterisation. The F-18-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 160degreesC. Hydrolysis is completed with 1N HCl at 50degreesC within 10 minutes without losses.

引用

页码：55 / 58

页数：4

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