NMPA Key Laboratory for Research and Evaluation of Innovative Drug, Henan Key Laboratory of Organic Functional Molecules and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China.
J Org Chem. 2021 Dec 17;86(24):18211-18223. doi: 10.1021/acs.joc.1c02497. Epub 2021 Nov 24.
We report herein the ()-3,3'-Br-BINOL-catalyzed enantioselective conjugate addition of organic boronic acids to β,γ-unsaturated α-ketoesters to generate the corresponding Michael addition products in moderate to high yields and with moderate to excellent enantioselectivities (up to 99% ). This catalytic system features characteristics of mild reaction conditions, high efficiency, and tolerance to alkenylboronic acids and heteroarylboronic acids.
我们在此报告了 ()-3,3'-Br-BINOL 催化的有机硼酸对β,γ-不饱和α-酮酯的对映选择性共轭加成反应，以中等至高等收率和中等至优异的对映选择性（高达 99%）生成相应的迈克尔加成产物。该催化体系具有反应条件温和、效率高、对烯基硼酸和杂芳基硼酸的耐受性的特点。
