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

页码：13963 / 13966

页数：4

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