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Intramolecular Appel Reaction of Trifluoromethylated β‑Keto Diazos Enabling Assembly of Trifluoromethylpyrazoles

Posted on 2022-03-17 - 12:33
A method for the generation of trifluoromethylated β-keto diazos and their applications in intramolecular Appel type reactions are reported. The key success of this reaction is a diazo species as an N-nucleophile in Appel reactions. This reaction is conducted under mild conditions and has a broad substrate scope, affording trifluoromethylpyrazoles in ≤94% yields. This protocol represents a new type of Appel reaction and also a new reaction mode of fluoro diazoalkanes.

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