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Palladium-Catalyzed Phosphonylation: Synthesis of C3‑, C4‑, and C5-Phosphonylated Pyrazoles

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journal contribution
posted on 01.11.2013, 00:00 by Gaël Tran, Domingo Gomez Pardo, Tomoki Tsuchiya, Stefan Hillebrand, Jean-Pierre Vors, Janine Cossy
A palladium-catalyzed cross-coupling between 3-, 4-, and 5-halo-pyrazoles and H-phosphonates, H-phosphinates, and secondary phosphine oxides has been developed. This coupling reaction constitutes the first general method allowing the introduction of a great diversity of phosphorus substituents on the different carbons of the pyrazole ring in a one-step process.