The Buchwald-Hartwig Amination After 25 Years

Angew Chem Int Ed Engl. 2019 Nov 25;58(48):17118-17129. doi: 10.1002/anie.201904795. Epub 2019 Sep 18.

Abstract

The Pd-catalyzed coupling of aryl (pseudo)halides and amines is one of the most powerful approaches for the formation of C(sp2 )-N bonds. The pioneering reports from Migita and subsequently Buchwald and Hartwig on the coupling of aminostannanes and aryl bromides rapidly evolved into general and practical tin-free protocols with broad substrate scope, which led to the establishment of what is now known as the Buchwald-Hartwig amination. This Minireview summarizes the evolution of this cross-coupling reaction over the course of the past 25 years and illustrates some of the most recent applications of this well-established methodology.

Keywords: amination; arenes; cross-coupling; palladium; reaction mechanisms.

Publication types

  • Review