Evaluation of 4-[18F]fluoro-1-butyne as a radiolabeled synthon for click chemistry with azido compounds

被引：6
作者：
Kim, Dong Hyun [1 ]
Choe, Yearn Seong [1 ]
Kim, Byung-Tae [1 ]
机构：
[1] Sungkyunkwan Univ, Sch Med, Ctr Mol & Cellular Imaging,Dept Nucl Med, Samsung Med Ctr,Samsung Biomed Res Inst, Seoul 135710, South Korea
来源：
APPLIED RADIATION AND ISOTOPES | 2010年 / 68卷 / 02期
关键词：
Click chemistry; Radiolabeled acetylene synthon; 4-[F-18]fluoro-1-butyne; Vinyl acetylene; POSITRON-EMISSION-TOMOGRAPHY; TERMINAL ALKYNES; IN-VITRO; CYCLOADDITION; ACID; FLUORINATION; ANALOG; PET;
D O I：
10.1016/j.apradiso.2009.11.003
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
Click chemistry is a useful approach for the preparation of novel radiopharmaceuticals. In this study, we evaluated 4-[F-18]fluoro-1-butyne as a radiolabeled synthon for click chemistry with azido compounds. Our results showed that nucleophilic substitution of 4-tosyloxy-1-butyne with K[F-18]F produces vinyl acetylene as well as 4-[F-18]fluoro-1-butyne, while the same reaction using 5-tosyloxy-1-pentyne gives exclusively 5-[F-18]fluoro-1-pentyne. Thus, omega-[F-18]fluoro-1-alkynes with chain lengths longer than four carbons may be better radiolabeled synthons for use in click chemistry. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：329 / 333
页数：5
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