Synthesis of (E)-5-[2-(tri-n-butylstannyl)vinyl] substituted 2′-deoxyuridine derivatives for use in halogenation and radiohalogenation reactions

被引：0
|
作者：
Yu, CS
Oberdorfer, F
机构：
[1] German Canc Res Ctr, Dept Radiopharmaceut Chem, D-69120 Heidelberg, Germany
[2] Univ Freiburg Klinikum, PET Zentrum, EUROPET GmbH, D-79106 Freiburg, Germany
来源：
SYNLETT | 2000年 / 01期
关键词：
terminal alkyne; stannylation; fluorodestannylation; radiohalogenation;
D O I：
暂无
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A facile synthesis is reported for 5-[2-(tri-n-butyl-stannyl)vinyl]-2'-deoxyuridine 1, starting from commercial 5-iodo-2'-deoxyuridine 2 via the stannylation reaction as the key step. The 3',5'-di-O-acetyl-N(3)-p-toluoyl-protected analog of 1, compound 9, was then prepared. Electrophilic fluorination of 9 with carrier-added [F-18]F-2 provided the desired (E) and (Z) fluorovinyl compounds 10, bur not as the major products. The E/Z ratio of 10 was 2:1. The main product of the reaction was the proton substituted compound 11.
引用
收藏
页码：86 / 88
页数：3
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