Dramatic Acceleration of an Acyl Transfer-Initiated Cascade by Using Electron-Rich Amidine-Based Catalysts

Org Lett. 2017 Dec 15;19(24):6486-6489. doi: 10.1021/acs.orglett.7b03044. Epub 2017 Dec 4.

Abstract

A tandem rearrangement of α,β-unsaturated thioesters into tricyclic ene-lactones fails with conventional amidine-based catalysts, but becomes possible when their electron-rich analogs are employed. A highly diastereo- and enantioselective version of this process has been developed using H-PIP 1b, a chiral catalyst prepared over a decade ago, but never utilized since its disclosure.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.