Small-molecule diversity using a skeletal transformation strategy

Org Lett. 2005 Jun 23;7(13):2535-8. doi: 10.1021/ol0504345.

Abstract

[reaction: see text] We describe a short synthetic sequence resulting in >4000 skeletally diverse small molecules that have three distinct skeletal frameworks among other unique structural features. The sequence entails skeletal transformations pioneered by Winterfeldt and co-workers. We use epoxide ring openings and subsequent functionalizations that provide, e.g., spirocyclic oxazolidines, Lewis acid catalyzed Diels-Alder reactions of a steroid-derived diene that afford stable and isolable ring B adducts, and subsequent retro-Diels-Alder fragmentations that yield 14-membered paracyclophanes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Catalysis
  • Combinatorial Chemistry Techniques / methods*
  • Cyclization
  • Indicators and Reagents
  • Molecular Structure
  • Polycyclic Aromatic Hydrocarbons / chemical synthesis*
  • Polycyclic Aromatic Hydrocarbons / chemistry*

Substances

  • Indicators and Reagents
  • Polycyclic Aromatic Hydrocarbons