Synthesis of (~(14)C-ring-(U))4-(trifluoromethyl)benzenesulfonyl chloride

摘要

[~(14)C-ring-(U)]4-(trifluoromethyl)benzenesulfonyl chloride (9) is a key intermediate in the synthesis of [~(14)C]-labeled drugs and can be prepared from [~(14)C-ring-(U)]4-(trifluoromethyl)phenylamine (8). The key step in the synthesis of 9 is the sulfonation of 8 meditated by a Sandmeyer-type reaction for the introduction of a sulfonyl group. Compound 9 can be synthesized from [~(14)C-ring-(U)]benzene via an eight-step process with an overall radiochemical yield of 20%.