Use of 2-[18F]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABAA receptor binding 4-quinolones

被引：21

作者：

Gaeta, Alessandra ^{[2
]}

Woodcraft, John ^{[2
]}

Plant, Stuart ^{[2
]}

Goggi, Julian ^{[2
]}

Jones, Paul ^{[2
]}

Battle, Mark ^{[2
]}

Trigg, William ^{[2
]}

Luthra, Sajinder K. ^{[1
,2
]}

Glaser, Matthias ^{[1
]}

机构：

[1] Hammersmith Hosp, GE Healthcare, London W12 0NN, England

[2] GE Healthcare, Amersham HP7 9LL, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

关键词：

Staudinger ligation; Click chemistry; GABA receptor; PET; Fluorine-18; POSITRON-EMISSION-TOMOGRAPHY; LIGANDS; PEPTIDE; AMIDE; AZIDE;

D O I：

10.1016/j.bmcl.2010.05.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The labelling reagent 2-[F-18]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABA(A) receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2-[F-18] fluoroethyl) amide. The radiotracer was prepared with a non-decay corrected radiochemical yield of 7%, a radiochemical purity >95% and a specific radioactivity of 0.9 GBq/mu mol. The compound showed low brain penetration in normal rats. A series of fluoroalkyl 4-quinolone analogues with nanomolar to sub-nanomolar affinity for the GABA(A) receptor has been prepared as well. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4649 / 4652

页数：4

共 25 条

[1] Fluorous Synthesis of 18F Radiotracers with the [18F]Fluoride Ion: Nucleophilic Fluorination as the Detagging Process [J].