Total Synthesis of Thailanstatin A

J Am Chem Soc. 2016 Jun 22;138(24):7532-5. doi: 10.1021/jacs.6b04781. Epub 2016 Jun 13.

Abstract

The total synthesis of the spliceosome inhibitor thailanstatin A has been achieved in a longest linear sequence of nine steps from readily available starting materials. A key feature of the developed synthetic strategy is the implementation of a unique, biomimetic asymmetric intramolecular oxa-Michael reaction/hydrogenation sequence that allows diastereodivergent access to highly functionalized tetrahydropyrans, which can be used for the synthesis of designed analogues of this bioactive molecule.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Chemistry Techniques, Synthetic / methods*
  • Drug Discovery
  • Hydrogenation
  • Molecular Structure
  • Pyrans / chemical synthesis*
  • Pyrans / chemistry
  • Pyrans / pharmacology
  • Spliceosomes / drug effects

Substances

  • Antineoplastic Agents
  • Pyrans
  • thailanstatin A