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[11C]Carbonyl Difluoride—a New and Highly Efficient [11C]Carbonyl Group Transfer Agent
Authors:Jimmy E Jakobsson  Shuiyu Lu  Sanjay Telu  Victor W Pike
Abstract:Herein, the synthesis and use of 11C]carbonyl difluoride for labeling heterocycles with 11C]carbonyl groups in high molar activity is described. A very mild single‐pass gas‐phase conversion of 11C]carbon monoxide into 11C]carbonyl difluoride over silver(II) fluoride provides easy access to this new synthon in robust quantitative yield for labeling a broad range of cyclic substrates, for example, imidazolidin‐2‐ones, thiazolidin‐2‐ones, and oxazolidin‐2‐ones. Labeling reactions may utilize close‐to‐stoichiometric precursor quantities and short reaction times at room temperature in a wide range of solvents while also showing high water tolerability. The overall radiosynthesis protocol is both simple and reproducible. The required apparatus can be constructed from widely available parts and is therefore well suited to be automated for PET radiotracer production. We foresee that this straightforward method will gain wide acceptance for PET radiotracer syntheses across the radiochemistry community.
Keywords:carbon-11  carbonyl difluoride  heterocycles  isotopic labeling  PET radiochemistry
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