Catalytic Asymmetric Synthesis of β,γ-Alkynyl α-Amino Esters via Chemo- and Enantio-selective Transfer Hydrogenation

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作者单位: Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, 250062, China College of Animal Science and Veterinary Medicine, Shandong Agricultural University, Tai'an, 271018, Shandong, China School of Chemistry and Chemical Engineering, Shandong University, Jinan, 250100, China

摘要: An effective chemo- and enantioselective transfer hydrogenation of β,γ-alkynyl α-imino esters to prepare optically pure β,γ-alkynyl α-amino esters has been described. The excellent chemoselectivity was achieved by using chiral phosphoric acid catalyzed asymmetric reduction with benzothiazoline as hydride donor. The reaction exhibited good functional group tolerance, providing a range of optically active non-natural amino esters with excellent enantioselectivity.

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