Organocatalyzed Enantioselective Conjugate Addition of Boronic Acids to β,γ-Unsaturated α-Ketoesters

• DOI: 10.1021/acs.joc.1c02497
• Publication Date: 2021-11-25T07:46:12Z
• Authors: Lu Zhao; En-Ze Yao; Guo-Li Chai; Shi-Yu Ma; Junbiao Chang
• Keywords: Conjugate; Addition reaction; Boronic acid

We report herein the (R)-3,3'-Br2-BINOL-catalyzed enantioselective conjugate addition of organic boronic acids to β,γ-unsaturated α-ketoesters generate corresponding Michael products in moderate high yields and with excellent enantioselectivities (up 99% ee). This catalytic system features characteristics mild reaction conditions, efficiency, tolerance alkenylboronic heteroarylboronic acids.