Synthesis 2018; 50(14): 2693-2706
DOI: 10.1055/s-0037-1610142
short review
© Georg Thieme Verlag Stuttgart · New York

Regioselective Transition-Metal-Catalyzed C–H Functionalization of Anilines

Jamie A. Leitch*
Department of Chemistry, University of Bath, Claverton Down, Somerset, BA2 7AY, UK   Email: j.leitch@bath.ac.uk   Email: c.g.frost@bath.ac.uk
,
Christopher G. Frost*
Department of Chemistry, University of Bath, Claverton Down, Somerset, BA2 7AY, UK   Email: j.leitch@bath.ac.uk   Email: c.g.frost@bath.ac.uk
› Author Affiliations
Further Information

Publication History

Received: 19 February 2018

Accepted after revision: 06 April 2018

Publication Date:
11 June 2018 (online)


Abstract

Anilines are a vital synthetic core of pharmaceuticals, agrochemicals, natural products and building blocks. Metal-catalyzed C–H functionalization has emerged as a powerful tool to derivatize biologically relevant molecules. To this end, the derivation of anilines via catalytic C–H functionalization has been the subject of important new synthetic methodology. This review focuses on the tactics used to allow regioselective C–H functionalization of anilines.

1 Introduction

2 ortho-Selective C–H Functionalization

2.1 Palladium

2.2 Rhodium

2.3 Ruthenium

2.4 Nickel

3 meta-Selective C–H Functionalization

4 para-Selective C–H Functionalization

5 Conclusion