Regioselective Spirostan E-Ring Opening for the Synthesis of Dihydropyran Steroidal Frameworks

Org Lett. 2016 Apr 15;18(8):1772-5. doi: 10.1021/acs.orglett.6b00492. Epub 2016 Mar 24.

Abstract

The regioselective opening of the ring E in spirostan sapogenins provides new dihydropyran derivatives. This novel side chain is obtained after a Lewis acid mediated acetolysis followed by an alkaline workup. The reaction mechanism is analyzed via density functional theory computations, and both experimental and computational data support the formation of an oxacarbenium intermediate. The behavior of the title skeletons under acidic conditions is also investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Lewis Acids / chemistry
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Pyrans / chemistry*
  • Spirostans / chemistry*
  • Stereoisomerism
  • Steroids / chemistry

Substances

  • Lewis Acids
  • Pyrans
  • Spirostans
  • Steroids