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

摘要

The 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.