Click for PET:: rapid preparation of [18F]fluoropeptides using CuI catalyzed 1,3-dipolar cycloaddition

被引：190

作者：

Marik, Jan ^{[1
]}

Sutcliffe, Julie L. ^{[1
]}

机构：

[1] Univ Calif Davis, Dept Biomed Engn, Davis, CA 95616 USA

来源：

TETRAHEDRON LETTERS | 2006年 / 47卷 / 37期

关键词：

D O I：

10.1016/j.tetlet.2006.06.176

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cu-I catalyzed 1,3-dipolar cycloaddition 'click chemistry' was used to prepare F-18-radiolabeled peptides. Three omega-[F-18]-fluoroalkynes were prepared in yields 1 ranging from 36% to 81%. Conjugation of omega-[F-18]fluoroalkynes to various peptides decorated with 3-azidopropionic acid via Cu-I mediated 1,3-dipolar cycloaddition yielded the desired F-18-labeled products in 10 min with yields of 54-99% and excellent radiochemical purity (81-99%). The total synthesis time was 30 min from the end of bombardment. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6681 / 6684

页数：4

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