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Catalytic Amination of 2-Substituted Pyridines with Hydrazine Derivatives

2001; American Chemical Society; Volume: 3; Issue: 9 Linguagem: Inglês

10.1021/ol015731y

1523-7060

Jeffrey B. Arterburn, Kalla Venkateswara Rao, Ranjit Ramdas, B.R. Dible,

Synthesis and Reactivity of Heterocycles

Protected pyridylhydrazine derivatives were prepared in a one-step palladium-catalyzed amination reaction using chelating phosphine ligands. 2-Pyridyl chlorides, bromides, and triflates were effective electrophiles in these reactions. Di-tert-butyl hydrazodiformate was an excellent hydrazine substrate, and the resulting products were deprotected under mild conditions. Catalytic amination provides a direct route to protected bifunctional hydrazinopyridine linkers that are suitable for metal-bioconjugate syntheses.