- Synthesis of18F-Difluoromethylarenes from Aryl (Pseudo) Halides
-
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 decay-corrected) from 10 to 60 %. The18F-fluorination precursors are readily prepared from aryl chlorides, bromides, iodides, and triflates. Seven18F-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.
- Shi, Hang,Braun, Augustin,Wang, Lu,Liang, Steven H.,Vasdev, Neil,Ritter, Tobias
-
supporting information
p. 10786 - 10790
(2016/09/03)
-
