Copper(I)‐Catalyzed Asymmetric Addition of Terminal Alkynes to β‐Imino Esters: An Efficient and Direct Method in the Synthesis of Chiral β3‐Alkynyl β2,2‐Dimethyl Amino Acid Derivatives

Abstract

Abstractmagnified imageThe first catalytic asymmetric addition of terminal alkynes to β‐imino esters was carried out using chiral copper(I) complexes as catalysts under mild reaction conditions, providing an efficient and direct synthetic approach to β3‐alkynyl β2,2‐dimethyl amino esters with yields of 73–97% and 48–90% ee. The rich chemistry of the alkynyl functionality makes the present method a powerful and versatile approach to a wide range of optically active β2,2‐dimethyl amino acid derivatives.