18F-Labeling of Aryl-SCF3, -OCF3 and -OCHF2 with [18F]Fluoride

被引：81
作者：
Khotavivattana, Tanatorn [1 ]
Verhoog, Stefan [1 ]
Tredwell, Matthew [1 ]
Pfeifer, Lukas [1 ]
Calderwood, Samuel [1 ]
Wheelhouse, Katherine [3 ]
Collier, Thomas Lee [2 ]
Gouverneur, Veronique [1 ]
机构：
[1] Univ Oxford, Chem Res Lab, Oxford OX1 3TA, England
[2] Advion BioSyst, Ithaca, NY 14850 USA
[3] GlaxoSmithKline R&D, Med Discovery & Dev, Stevenage SG1 2NY, Herts, England
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2015年 / 54卷 / 34期
基金：
英国工程与自然科学研究理事会;
关键词：
F-18]fluoride; difluoromethyl ethers; halogen exchange; silver triflate; trifluoromethyl ethers; OXIDATIVE DESULFURIZATION-FLUORINATION; ETHER METAL FLUORIDE; ARYL BORONIC ACIDS; TRIFLUOROMETHYL ETHERS; BINDING-ENERGIES; LATE-STAGE; CATALYZED SYNTHESIS; SILVER ION; F-18; PET;
D O I：
10.1002/anie.201504665
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
We report that halogenophilic silver(I) triflate permits halogen exchange (halex) nucleophilic F-18-fluorination of aryl-OCHFCl, -OCF2Br and -SCF2Br precursors under mild conditions. This Ag-I-mediated process allows for the first time access to a range of F-18-labeled aryl-OCHF2, -OCF3 and -SCF3 derivatives, inclusive of [F-18]riluzole. The F-18-labeling of these medicinally important motifs expands the radiochemical space available for PET applications.
引用
收藏
页码：9991 / 9995
页数：5
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