Reversal of Enantioselectivity in the Copper-Aminophenol Sulfonamide Catalyzed Alkynylation of Isatins by Slightly Tuning the Ligand Structure and Basic Additives

Org Lett. 2021 Aug 6;23(15):5739-5743. doi: 10.1021/acs.orglett.1c01896. Epub 2021 Jul 19.

Abstract

A series of new chiral aminophenol sulfonamide ligands with a monochiral arm has been developed for the first Cu(I) catalyzed enantiodivergent alkynylation of isatins. Dramatic reversal of enantioselectivity was accomplished by slightly tuning the substituted benzenesulfonamide and achiral basic additives. A wide range of both terminal alkynes and isatins are tolerated by this new catalyst system with up to 99% yield and 97% ee.

Publication types

  • Research Support, Non-U.S. Gov't