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Synthesis of N-Arylpyrazoles by Palladium-Catalyzed Coupling of Aryl Triflates with Pyrazole Derivatives

Shunsuke Onodera, Takuya Kochi, Fumitoshi Kakiuchi*

*Department of Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, Kanagawa 223-8522, Japan, Email:

S. Onodera, T. Kochi, F. Kakiuchi, J. Org. Chem., 2019, 84, 6508-6515.

DOI: 10.1021/acs.joc.9b00673

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A palladium-catalyzed coupling of aryl triflates with pyrazole derivatives using tBuBrettPhos as a ligand provides N-arylpyrazoles in very good yields. The coupling products of 3-trimethylsilylpyrazole served as a useful template for syntheses of further N-arylpyrazole derivatives.

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Key Words

N-arylation, pyrazoles

ID: J42-Y2019