Development, Optimization, and Scope of the Radiosynthesis of 3/5-[18F]Fluoropyridines from Readily Prepared Aryl(pyridinyl) Iodonium Salts: The Importance of TEMPO and K2CO3

doi:10.1021/ACS.OPRD.9B00021

Paper

Development, Optimization, and Scope of the Radiosynthesis of 3/5-[18F]Fluoropyridines from Readily Prepared Aryl(pyridinyl) Iodonium Salts: The Importance of TEMPO and K2CO3

Published Apr 11, 2019 · M. Pauton, C. Aubert, G. Bluet

Organic Process Research & Development

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10

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Abstract

A robust process for the radiosynthesis of 3/5-[18F]fluoropyridines has been developed by radiofluorination of iodonium triflates using K18F/K2CO3/K222 complex in the presence of TEMPO. Both electronically deficient and enriched iodonium salts were readily obtained from the corresponding 3/5-iodopyridines and afforded the corresponding 3/5-[18F]fluoropyridines in 6–78% yields. The concentrations of K2CO3 and TEMPO were found to be crucial for the radiofluorination efficiency. The process was validated using two automated systems for the 18F-radiolabeling of 2-chloro and 2-carboxamido-5-fluoropyridines carried out in 10–20% yields.

Study Snapshot

The developed process for radiosynthesis of 3/5-[18F]fluoropyridines from iodonium triflates with TEMPO and K2CO3 is efficient and can produce 6-78% yields, with K2CO3 and TEMPO concentrations being crucial for radiofluorination efficiency

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Development, Optimization, and Scope of the Radiosynthesis of 3/5-[18F]Fluoropyridines from Readily Prepared Aryl(pyridinyl) Iodonium Salts: The Importance of TEMPO and K2CO3

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