Facile purification and click labeling with 2-[18F]fluoroethyl azide using solid phase extraction cartridges

Dong Zhou; Wenhua Chu; Xin Peng; Jonathan McConathy; Robert H Mach; John A Katzenellenbogen

doi:10.1016/j.tetlet.2014.10.126

Facile purification and click labeling with 2-[¹⁸F]fluoroethyl azide using solid phase extraction cartridges

Tetrahedron Lett. 2015 Feb 7;56(7):952-954. doi: 10.1016/j.tetlet.2014.10.126. Epub 2014 Nov 4.

Authors

Dong Zhou¹, Wenhua Chu¹, Xin Peng¹, Jonathan McConathy¹, Robert H Mach¹, John A Katzenellenbogen²

Affiliations

¹ Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 S. Kingshighway Blvd., St Louis, MO 63110, USA.
² Department of Chemistry, University of Illinois, Urbana, IL 61801, USA.

Abstract

A facile method was developed to purify 2-[¹⁸F]fluoroethyl azide ([¹⁸F]FEA) using a C18 cartridge and an Oasis^® HLB cartridge in series, in which [¹⁸F]FEA was exclusively trapped on the HLB cartridge. [¹⁸F]FEA can be eluted for reactions in solution; alternatively click labeling can be carried out on the HLB cartridge itself by loading an alkyne substrate and copper (I) catalyst dissolved in DMF onto the cartridge. This solid phase extraction methodology for purification and click labeling with [¹⁸F]FEA, either in solution or on the cartridge, is safe, simple, reproducible in high yield, and compatible with automated synthesis of ¹⁸F-labeled PET tracers.

Keywords: 2-Fluoroethyl azide; Click chemistry; Fluorine-18; Positron emission tomography; Radiolabeling; Solid phase extraction.

Abstract

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