Abstract

AbstractThe synthesis of 2‐[18F]trifluoromethylated indoles from the corresponding chlorodifluoromethyl precursors was found to proceed under milder conditions when compared to known metal‐free nucleophilic exchange reactions with [18F]fluoride on chlorodifluoro‐methyl arenes. A key element in the reaction course is – most likely – a favorable elimination‐addition mechanism on the 2‐methyl position of the indole. Given the increasing interest in 18F‐labelled compounds, this single step labeling methodology nicely complements the so far existing routes to 2‐[18F]trifluoromethylated indoles.

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