Synlett 2023; 34(19): 2336-2340
DOI: 10.1055/a-2158-1015
letter

Metal-Free Catalyzed Defluorinative O-Arylation of Pyrazolones with Polyfluoroarenes

Liu Yang
,
Tao Qin
,
Bin Liu
This work was supported by the National Natural Science Foundation of China (No. 22201158) and the Higher Education Discipline Innovation Project (111 Project of China, No. D20015).


Abstract

An efficient and general method for defluorinative O-arylation of pyrazolones has been successfully developed under metal-free conditions. This methodology allows for the synthesis of desired products by using a wide range of pyrazolones and polyfluoroarenes as starting materials. The compatibility of various substrates was demonstrated, ensuring the applicability of this method. Furthermore, the synthesis of the target compounds at a gram scale and the ability to perform late-stage modifications highlight the potential of this approach in preparative pharmaceutical synthesis and organofluorine chemistry.

Supporting Information



Publikationsverlauf

Eingereicht: 24. Juli 2023

Angenommen nach Revision: 22. August 2023

Accepted Manuscript online:
22. August 2023

Artikel online veröffentlicht:
27. September 2023

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