Transition-Metal-Free N-Arylation of Pyrazoles with Diaryliodonium Salts

Abstract

A new synthetic method was developed for the N-arylation of pyrazoles using diaryliodonium salts. The transformation does not require any transition-metal catalyst and provides the desired N-arylpyrazoles rapidly under mild reaction condition in the presence of aqueous ammonia solution as a mild base without the use of inert atmosphere. The chemoselectivity of unsymmetric diaryliodonium salts was also explored with large number of examples.

Keywords: amination; heterocycles; iodonium salts; pyrazoles.