Late-Stage 18 F/ 19 F Isotopic Exchange for the Synthesis of 18 F-Labeled Sulfamoyl Fluorides
Authors
Min Ho Jeon ; Young-Do Kwon ; Min Pyeong Kim ; Gianluca Bartolini Torres ; Jeong Kon Seo ; Jeongmin Son ; Young Hoon Ryu ; Sung You Hong ; Joong-Hyun Chun
Synthesis of sulfamoyl [18F]fluorides has been a challenging topic owing to the inefficient nucleophilic radiofluorination of sulfamoyl derivatives. Herein, we report an 18F/19F isotopic exchange approach to synthesize various sulfamoyl [18F]fluorides, otherwise inaccessible via direct synthesis from amines, with high radiochemical yields up to 97% (30 examples). This late-stage labeling protocol offers an efficient route to yield functionalized molecules by diversifying the chemical library possessing sulfamoyl functionalities through nucleophilic 18F incorporation within nitrogen-containing sulfur(VI) frameworks.