Copper-Catalyzed Amino-alkoxycarbonylation of Unactivated Alkenes: Synthesis of β‑Amino Esters via Primary Tosyl Amidyl Radical

TL;DR

The paper introduces a new copper-catalyzed method to efficiently synthesize β-amino esters from unactivated alkenes using a primary tosyl amidyl radical.

Contribution

A novel copper-catalyzed amino-alkoxycarbonylation method for synthesizing β-amino esters from unactivated alkenes.

Findings

A primary tosyl amidyl radical initiates 1,2-amino-alkoxycarbonylation of unactivated alkenes.

The method provides a straightforward and efficient synthesis of β-amino acid derivatives.

Abstract

β-Amino acids
serve as essential motifs in a wide array of
bioactive compounds, pharmaceuticals, and natural products, playing
a crucial role in the development of peptides and peptidomimetics.
Transition-metal-catalyzed carbonylative functionalization represents
an ideal strategy for synthesizing carbonyl-containing compounds.
In this context, we disclose a primary tosyl amidyl radical initiated
1,2-amino-alkoxycarbonylation of unactivated alkenes, which offers
a straightforward and efficient approach to synthesize β-amino
acid derivatives.

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