Methods for Arylethylation of Amines and Heteroarenes

Abstract

Compared with standard N-methylation, benzylation, and alkylation of amines and N-heterocycles, N-arylethylation is significantly more challenging. In this Review the available methods for N-arylethylation are summarized, with a special focus on efficiency, selectivity, availability of the required building blocks, and ecological aspects.

Photoinduced Copper-Catalyzed Late-Stage Azidoarylation of Alkenes via Arylthianthrenium Salts

“…The widespread use as a pharmacophore has motivated extensive research into syntheses of β-arylethylamines (Figures A and S1). Conventional methods to prepare them often employ indirect and multistep sequences, such as homologation and reductive amination . Over the past few decades, a variety of synthetic methods have been developed, of which 1,2-aminoarylation of alkenes is a promising and straightforward approach because of the direct utilization of readily available arenes, alkenes, and amines .…”