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Schlagwörter:
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Zusammenfassung:
A general method for the synthesis of
[18F]difluoromethylarenes from [18F]fluoride for radiopharmaceutical
discovery is reported. The method is practical,
operationally simple, tolerates a wide scope of functional
groups, and enables the labeling of a variety of arenes and
heteroarenes with radiochemical yields (RCYs, not decaycorrected)
from 10 to 60%. The 18F-fluorination precursors are
readily prepared from aryl chlorides, bromides, iodides, and
triflates. Seven 18F-difluoromethylarene drug analogues and
radiopharmaceuticals including Claritin, fluoxetine (Prozac),
and [18F]DAA1106 were synthesized to show the potential of
the method for applications in PET radiopharmaceutical
design.
