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.