The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography

Abstract

A range of resin bound sulfonate ester linkers were developed for use in the resin-linker-vector (RLV) approach for the synthesis of [18F]-fluoride radiotracers for use as imaging agents in positron-emission-tomography (PET). The RLV strategy immobilises a precursor to the desired radiotracer on a solid support which is cleaved on exposure to [18F]-fluoride ion to give the 18F-labelled radiotracer in solution. The RLV methodology allows for easier purification of the 18F-labelled radiotracer as a simple filtration step removes the unreacted starting material and the cleaved resin.

Synthetic routes to a 4-allkylphenylsulfonate linker and a 4-nitrophenylsulfonate linker were developed and these were shown to work as desired as part of the RLV construct in [19F]-fluoridolysis reactions. [18F]-Fluoridolysis reactions using the 4-alkylphenylsulfonate linker gave the desired 18F-labelled product in excellent radiochemical purity. The RLV strategy with this linker type was applied in a new synthetic route to O-(2-[18F]-fluoroethyl)-L-tyrosine.

A fluorinated analogue of Alzheimer’s disease drug (?)-galanthamine was synthesised with complete stereocontrol as a potential new imaging agent for use in PET.

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Identifiers

ORCID for Richard C.D. Brown: orcid.org/0000-0003-0156-7087

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