Late-Stage F-18/F-19 Isotopic Exchange for the Synthesis of F-18-Labeled Sulfamoyl Fluorides
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- Late-Stage F-18/F-19 Isotopic Exchange for the Synthesis of F-18-Labeled Sulfamoyl Fluorides
- Jeon, Min Ho; Kwon, Young-Do; Kim, Min Pyeong; Torres, Gianluca Bartolini; Seo, Jeong Kon; Son, Jeongmin; Ryu, Young Hoon; Hong, Sung You; Chun, Joong-Hyun
- Issue Date
- AMER CHEMICAL SOC
- ORGANIC LETTERS, v.23, no.7, pp.2766 - 2771
- Synthesis of sulfamoyl [F-18]fluorides has been a challenging topic owing to the inefficient nucleophilic radiofluorination of sulfamoyl derivatives. Herein, we report an F-18/F-19 isotopic exchange approach to synthesize various sulfamoyl [F-18]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 F-18 incorporation within nitrogen-containing sulfur(VI) frameworks.
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