Efficient DBU accelerated synthesis of 18F-labelled trifluoroacetamides

被引：12
|
作者：
Gomez, Antonio Bermejo [1 ,2 ,3 ]
Gonzalez, Miguel A. Cortes [2 ,3 ]
Lubcke, Marvin [2 ,3 ]
Johansson, Magnus J. [4 ]
Halldin, Christer [3 ,5 ]
Szabo, Kalman J. [2 ,3 ]
Schou, Magnus [1 ,3 ,5 ]
机构：
[1] Karolinska Univ Sjukhuset Solna, Karolinska Inst, PET Ctr, AstraZeneca Personalised Healthcare & Biomarkers, R5 02, SE-17176 Stockholm, Sweden
[2] Stockholm Univ, Dept Organ Chem, Arrhenius Lab, SE-10691 Stockholm, Sweden
[3] Karolinska Inst, Stockholm Brain Inst, SE-17177 Stockholm, Sweden
[4] Med Chem AstraZeneca R&D, CVMD iMed, SE-43183 Molndal, Sweden
[5] Karolinska Inst, Dept Clin Neurosci, S-17176 Stockholm, Sweden
来源：
CHEMICAL COMMUNICATIONS | 2016年 / 52卷 / 97期
基金：
瑞典研究理事会;
关键词：
POSITRON-EMISSION-TOMOGRAPHY; ARYL IODIDES; FLUORINE; HETEROARENES; ARENES; PHARMACEUTICALS; DERIVATIVES; TRIFLATE; ALKENES; AGENT;
D O I：
10.1039/c6cc08535k
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Nucleophilic F-18-fluorination of bromodifluoromethyl derivatives was performed using [F-18] Bu4NF in the presence of DBU(1,8-diazabicyclo[5.4.0]undec-7-ene). This novel procedure provided a diverse set of [F-18] trifluoroacetamides in good to excellent radiochemical conversions. A mechanism where DBU acts as organomediator in this transformation is proposed.
引用
收藏
页码：13963 / 13966
页数：4
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