Short, Divergent, and Enantioselective Total Synthesis of Bioactive ent-Pimaranes

Org Lett. 2022 Oct 7;24(39):7151-7156. doi: 10.1021/acs.orglett.2c02843. Epub 2022 Sep 28.

Abstract

We present the first total synthesis of eight ent-pimaranes via a short and enantioselective route (11-16 steps). Key features of the divergent synthesis are a Sharpless asymmetric dihydroxylation, a Brønsted acid catalyzed cationic bicyclization, and a mild Rh-catalyzed arene hydrogenation for rapid access to a late synthetic branching point. From there on, selective functional group manipulations enable the synthesis of ent-pimaranes bearing different modifications in the A- and C-rings.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abietanes*
  • Hydrogenation
  • Hydroxylation
  • Rhodium*
  • Stereoisomerism

Substances

  • Abietanes
  • Rhodium