Hexafluoroisopropanol‐Enabled One‐Step Access to Oxetanol and Azetidinol Scaffolds from Unprotected Indoles and Heteroarenes
Abstract
This work reports a direct, hexafluoroisopropanol (HFIP)‐enabled, one‐step construction of oxetanol and azetidinol scaffolds from unprotected indoles and other electron‐rich (hetero)arenes via selective activation of strained four‐membered heterocyclic ketones. The method operates under mild, protecting‐group‐free conditions, shows broad functional‐group tolerance (e.g., halides, ester, boronate), and accommodates diversely substituted indoles. Compared with metal–halogen activation routes, this approach streamlines access to valuable strained tertiary‐alcohol frameworks with strong potential for late‐stage functionalization in medicinal chemistry.
Fields of Study & Subjects
Catalytic C–H Functionalization Methods
Synthesis and Catalytic Reactions
Cyclopropane Reaction Mechanisms
Publication details
- Journal / source
- Advanced Synthesis & Catalysis
- Publisher
- Wiley
- Volume
- 368
- Issue
- 3
- Publication date
- 3 February 2026
- Language
- EN