Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Toshima-ku, Tokyo 171-8588, Japan.
J Org Chem. 2023 Jun 16;88(12):7774-7783. doi: 10.1021/acs.joc.2c02633. Epub 2023 Apr 12.
We have developed a chiral phosphoric acid-catalyzed enantioselective Friedel-Crafts alkylation reaction between pyrroles and indolylmethanols. Wide substrate scope was observed, and a chiral all-carbon quaternary center was constructed at the 3 position of indoles in high yields with high to excellent enantioselectivities (up to 99% ee).
我们开发了一种手性磷酸催化的吡咯和吲哚甲醇之间的对映选择性 Friedel-Crafts 烷基化反应。观察到了广泛的底物范围，并以高产率和高至优异的对映选择性（高达 99%ee）构建了吲哚 3 位的手性全碳季碳中心。
