In:
Molecules, MDPI AG, Vol. 26, No. 18 ( 2021-09-11), p. 5522-
Abstract:
In this report, a simple and efficient process to achieve fluorine-18-labeled 1,2,3-triazole is reported. The heteroaromatic radiofluorination was successfully achieved through an iodine–fluorine-18 exchange in an aqueous medium requiring only trace amounts of base and no azeotropic drying of fluorine-18. This methodology was optimized on a model reaction and further validated on multiple 1,2,3-triazole substrates with 18–60% radiochemical conversions. Using this strategy—the radiosynthesis of a triazole-based thiamin analogue—a potential positron emission tomography (PET) probe for imaging thiamin-dependent enzymes was synthesized with 10–16% isolated radiochemical yield (RCY) in 40 min (uncorrected, n 〉 5).
Type of Medium:
Online Resource
ISSN:
1420-3049
DOI:
10.3390/molecules26185522
Language:
English
Publisher:
MDPI AG
Publication Date:
2021
detail.hit.zdb_id:
2008644-1
