Catalytic Enantioselective Synthesis of 3,4-Polyfused Oxindoles with Quaternary All-Carbon Stereocenters: A Rh-Catalyzed C-C Activation Approach

Org Lett. 2018 Dec 7;20(23):7689-7693. doi: 10.1021/acs.orglett.8b03412. Epub 2018 Nov 29.

Abstract

The first Rh-catalyzed enantioselective synthesis of a 3,4-polyfused oxindole ring system enabled by carboacylation of acrylic amides based on C-C activation is reported. This transformation provides a new entry to access 3,4-polyfused oxindoles bearing quaternary stereocenters. Tri- to pentacyclic 3,4-fused oxindoles were asymmetrically generated in good yields (up to 95%) with good to excellent enantioselectivity (88%-97% ee). Application in the first total synthesis of xylanigripones A was completed in 6 steps with a 14% overall yield.

Publication types

  • Research Support, Non-U.S. Gov't